6-membered aromatics as factor Xa inhibitors

ABSTRACT

The present application describes 6-membered aromatics of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein D may be CH 2  NH 2  or C(═NH)NH 2 , which are useful as inhibitors of factor Xa.

This application claims the benefit of U.S. Provisional Application No. 60/050,214, filed Jun. 19, 1997.

FIELD OF THE INVENTION

This invention relates generally to novel 6-membered aromatics which are inhibitors of trypsin-like serine protease enzymes, especially factor Xa, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.

BACKGROUND OF THE INVENTION

WO 96/28427 describes benzamidine anticoagulants of the formula: ##STR2## wherein Z¹ and Z² are O, N(R), S or OCH₂ and the central ring may be phenyl or a variety of heterocycles. The presently claimed compounds do not contain the Z¹ linker or the substitution pattern of the above compounds.

WO 95/18111 addresses fibrinogen receptor antagonists, containing basic and acidic termini, of the formula: ##STR3## wherein R¹ represents the basic termini, U is an alkylene or heteroatom linker, V may be a heterocycle, and the right hand portion of the molecule represents the acidic termini. The presently claimed compounds do not contain the acidic termini of WO 95/18111.

Activated factor Xa, whose major practical role is the generation of thrombin by the limited proteolysis of prothrombina holds a central position that links the intrinsic and extrinsic activation mechanisms in the final common pathway of blood coagulation. The generation of thrombin, the final serine protease in the pathway to generate a fibrin clot, from its precursor is amplified by formation of prothrombinase complex (factor Xa, factor V, Ca²⁺ and phospholipid). Since it is calculated that one molecule of factor Xa can generate 138 molecules of thrombin (Elodi, S., Varadis K.: Optimization of conditions for the catalytic effect of the factor IXa-factor VIII Complex: Probable role of the complex in the amplification of blood coagulation. Thromb. Res. 1979, 15, 617-629), inhibition of factor Xa may be more efficient than inactivation of throibin in interrupting th e blood coagulation system.

Therefore, efficacious and specific inhibitors of factor Xa are needed as potentially valuable therapeutic agents for the treatment of thromboembolic disorders. It is thus desirable to discover new factor Xa inhibitors.

SUMMARY OF THE INVENTION

Accordingly, one object of the present invention is to provide novel 6-membered aromatics which are useful as factor Xa inhibitors or pharmaceutically acceptable salts or prodrugs thereof.

It is another object of the present invention to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt or prodrug form thereof.

It is another object of the present invention to provide a method for treating thromboembolic disorders comprising administering to a host in need of such treatment a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt or prodrug form thereof.

These and other objects, which will become apparent during the following detailed description, have been achieved by the inventors' discovery that compounds of formula (I): ##STR4## or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, D, E, M, R^(1a), R^(1b), and Z are defined below, are effective factor Xa inhibitors.

DETAILED DESCRIPTION OF PREFERRED EMBODIMENTS

[1] Thus, in a first embodiment, the present invention provides novel compounds of formula I: ##STR5## or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein;

ring M contains from 0-4 N atoms;

D is selected from CN, C(═NR⁷)NR⁸ R⁹, NHC(═NR⁷)NR⁸ R⁹, NR⁸ CH(═NR⁷), C(O)NR⁸ R⁹, and (CR⁸ R⁹)_(t) NR⁸ R⁹ ;

E is selected from phenyl, 2-pyridyl, 4-pyridyl, pyrimidyl, and piperidinyl substituted with 1 R;

R is selected from H, F, Cl, Br, I, OR³, SR³, CO₂ R³, NO₂, and CH₂ OR³, and (CR⁸ R⁹)_(t) NR⁸ R⁹ ;

alternatively, E and R combine to form methylenedioxy or ethylenedioxy;

Z is selected from a bond, C₁₋₄ alkylene, (CH₂)_(r) O(CH₂)_(r), (CH₂)_(r) NR³ (CH₂)_(r), (CH₂)_(r) C(O)(CH₂)_(r), (CH₂)_(r) C(O)O(CH₂)_(r), (CH₂)_(r) OC(O) (CH₂)_(r), (CH₂)_(r) C(O)NR³ (CH₂)_(r), (CH₂)_(r) NR³ C(O)(CH₂)_(r), (CH₂)_(r) OC(O)O(CH₂)_(r), (CH₂)_(r) OC(O)NR³ (CH₂)_(r), (CH₂)_(r) NR³ C(O)O(CH₂)_(r), (CH₂)_(r) NR³ C(O)NR³ (CH₂)_(r), (CH₂)_(r) S(O)p(CH₂)_(r), (CH₂)_(r) SO₂ NR³ (CH₂)_(r), (CH₂)_(r) NR³ SO₂ (CH₂)_(r), and (CH₂)_(r) NR³ SO₂ NR³ (CH₂)_(r), provided that Z does not form a N--N, N--O, N--S, NCH₂ N, NCH₂ O, or NCH₂ S bond with ring M or group A;

R^(1a) and R^(1b) are independently absent or selected from --(CH₂)_(r) --R^(1'), --CH═CH--R^(1'), NCH₂ R^(1"), OCH₂ R^(1"), SCH₂ R^(1"), NH(CH₂)₂ (CH₂)_(t) R^(1'), O(CH₂)₂ (CH₂)_(R) ^(1'), and S(CH₂)₂ (CH₂)_(R) ^(1') ;

alternatively, R^(1a) and R^(1b), when attached to adjacent carbon atoms, together with the atoms to which they are attached form a 5-8 membered saturated, partially saturated or unsaturated ring substituted with 0-2 R⁴ and which contains from 0-2 heteroatoms selected from the group consisting of N, O, and S;

alternatively, when Z is C(O)NH and R^(1a) is attached to a ring carbon adjacent to Z, then R^(1a) is a C(O) which replaces the amide hydrogen of Z to form a cyclic imide;

R^(1') is selected from H, C₁₋₃ alkyl, F, Cl, Br, I, --CN, --CHO, (CF₂)_(r) CF₃, (CH₂)_(r) OR², NR² R^(2a), C(O)R^(2c), OC(O)R², (CF₂)_(r) CO₂ R^(2c), S(O)_(p) R^(2b), NR² (CH₂)_(r) OR², CH(═NR^(2c))NR² R^(2a), NR² C(O)R^(2b), NR² C(O)NHR^(2b), NR² C(O)₂ R^(2a), OC(O)NR^(2a) R^(2b), C(O)NR² R^(2a), C(O)NR² (CH₂)_(r) OR², SO₂ NR² R^(2a), NR² SO₂ R^(2b), C₃₋₆ carbocyclic residue substituted with 0-2 R⁴, and 5-10 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R⁴ ;

R^(1") is selected from H, CH(CH₂ OR²)₂, C(O)R^(2c), C(O)NR² R^(2a), S(O)R^(2b), S(O)₂ R^(2b), and SO₂ NR² R^(2a) ;

R², at each occurrence, is selected from H, CF₃, C₁₋₆ alkyl, benzyl, C₃₋₆ carbocyclic residue substituted with 0-2 R^(4b), and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R^(4b) ;

R^(2a), at each occurrence, is selected from H, CF₃, C₁₋₆ alkyl, benzyl, phenethyl, C₃₋₆ carbocyclic residue substituted with 0-2 R^(4b), and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R^(4b) ;

R^(2b), at each occurrence, is selected from CF₃, C₁₋₄ alkoxy, C₁₋₆ alkyl, benzyl, C₃₋₆ carbocyclic residue substituted with 0-2 R^(4b), and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R^(4b) ;

R^(2c), at each occurrence, is selected from CF₃, OH, C₁₋₄ alkoxy, C₁₋₆ alkyl, benzyl, C₃₋₆ carbocyclic residue substituted with 0-2 R^(4b), and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R^(4b) ;

alternatively, R² and R^(2a), together with the atom to which they are attached, combine to form a 5 or 6 membered saturated, partially saturated or unsaturated ring substituted with 0-2 R^(4b) and containing from 0-1 additional heteroatoms selected from the group consisting of N, O, and S;

R³, at each occurrence, is selected from H, C₁₋₄ alkyl, and phenyl;

R^(3a), at each occurrence, is selected from H, C₁₋₄ alkyl, and phenyl;

R^(3b), at each occurrence, is selected from H, C₁₋₄ alkyl, and phenyl;

R^(3c), at each occurrence, is selected from C₁₋₄ alkyl, and phenyl;

A is selected from:

C₃₋₁₀ carbocyclic residue substituted with 0-2 R⁴, and

5-10 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R⁴ ;

B is selected from: H, Y, and X--Y;

X is selected from C₁₋₄ alkylene, --CR² (CR² R^(2b)) (CH₂)_(t) --, --C(O)--, --C(═NR¹)--, --CR² (NR^(1") R²)--, --CR² (OR²)--, --CR² (SR²)--, --C(O)CR² R^(2a) --, --CR² R^(2a) C(O), --S(O)_(p) --, --S(O)_(p) CR² R^(2a) --, --CR² R^(2a) S(O)_(p) --, S(O)₂ NR² --, --NR² S(O)₂ --, --NR² S(O)₂ CR² R^(2a) --, CR² R^(2a) S(O)₂ NR² --, --NR² S(O)₂ NR² --, --C(O)NR² --, --NR² C(O)--, --C(O)NR^(2c) R² R^(2a) --, ,NR² C(O)CR² R^(2a) --, --CR² R^(2a) C(O)NR² --, --CR² R^(2a) NR² C(O)--, --NR² C(O)O--, --OC(O)NR² --, --NR² C(O)NR² --, --NR² --, --NR² CR² R^(2a) --, --CR² R^(2a) NR² --, O, --CR² R^(2a) O--, and --OCR² R^(2a) --;

Y is selected from:

(CH₂)_(r) NR² R^(2a), provided that X--Y do not form a N--N, O--N, or S--N bond,

C₃₋₁₀ carbocyclic residue substituted with 0-2 R^(4a), and

5-10 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R^(4a) ;

R⁴, at each occurrence, is selected from H, ═O, (CH₂)_(r) OR², F, Cl, Br, I, C₁₋₄ alkyl, --CN, NO₂, (CH₂)_(r) NR² R^(2a), (CH₂)_(r) C(O)R^(2c), NR² C(O)R^(2b), C(O)NR² R^(2a), NR² C(O)NR² R^(2a), CH(═NR²)NR² R^(2a), CH(═NS(O)₂ R⁵)NR² R^(2a), NHC(═NR²)NR² R^(2a), C(O)NHC(═NR²)NR² R^(2a), SO₂ NR² R^(2a), NR² SO₂ NR² R^(2a), NR² SO₂ -C₁₋₄ alkyl, NR² SO₂ R⁵, S(O)_(p) R⁵, (CF₂)_(r) CF₃, NCH₂ R^(1"), OCH₂ R^(1"), SCH₂ R^(1"), N(CH₂)₂ (CH₂)_(t) R^(1'), O(CH₂)₂ (CH₂)_(t) R^(1"), and S(CH₂)₂ (CH₂)_(t) R^(1') ;

alternatively, one R⁴ is a 5-6 membered aromatic heterocycle containing from 1-4 heteroatoms selected from the group consisting of N, O, and S;

R^(4a), at each occurrence, is selected from H, ═O, (CH₂)_(r) OR², (CH₂)_(r) --F, (CH₂)_(r) --Br, (CH₂)_(r) --Cl, I, C₁₋₄ alkyl, --CN, NO₂, (CH₂)_(r) NR² R^(2a), (CH₂)_(r) NR² R^(2b), (CH₂)_(r) C(O)R^(2c), NR² C(O)R^(2b), C(O) NR² R^(2a), C(O) NH(CH₂)₂ NR² R^(2a), NR² C(O)NR² R^(2a), CH(═NR²)NR² R^(2a), NHC(═NR²)NR² R^(2a), SO₂ NR² R^(2a), NR² SO₂ NR² NR^(2a), NR² SO₂ -C₁₋₄ alkyl, C(O)NHSO₂ -C₁₋₄ alkyl, NR² SO₂ R⁵, S(O)_(p) R⁵, and (CF₂)_(r) CF₃ ;

alternatively, one R^(4a) is a 5-6 membered aromatic heterocycle containing from 1-4 heteroatoms selected from the group consisting of N, O, and S and substituted with 0-1 R⁵ ;

R^(4b), at each occurrence, is selected from H, ═O, (CH₂)_(r) OR³, F, Cl, Br, I, C₁₋₄ alkyl, --CN, NO₂, (CH₂)_(r) NR³ R^(3a), (CH₂)_(r) C(O)R³, (CH₂)_(r) C(O)OR^(3c), NR³ C(O)R^(3a), C(O)NR³ R^(3a), NR³ C(O) NR³ R^(3a), CH(═NR³)NR³ R^(3a), NH₃ C(═NR³)NR³ R^(3a), SO₂ NR³ R^(3a), NR³ SO₂ NR³ R^(3a), NR³ SO₂ -C₁₋₄ alkyl, NR³ SO₂ CF₃, NR³ SO₂ -phenyl, S(O)_(p) CF₃, S(O)_(p) -C₁₋₄ alkyl, S(O)_(p) -phenyl, and (CF₂)_(r) CF₃ ;

R⁵, at each occurrence, is selected from CF₃, C₁₋₆ alkyl, phenyl substituted with 0-2 R⁶, and benzyl substituted with 0-2 R⁶ ;

R⁶, at each occurrence, is selected from H, OH, (CH₂)_(r) OR², F, Cl, Br, I, C₁₋₄ alkyl, CN, NO₂, (CH₂)_(r) NR² R^(2a), (CH₂)_(r) C(O)R^(2b), NR² C(O)R^(2b), NR² C(O)NR² R^(2a), CH(═NH)NH₂, NHC(═NH)NH₂, SO₂ NR² R^(2a), NR² SO₂ NR² R^(2a), and NR² SO₂ C₁₋₄ alkyl;

R⁷, at each occurrence, is selected from H, OH, C₁₋₆ alkyl, C₁₋₆ alkylcarbonyl, C₁₋₆ alkoxy, C₁₋₄ alkoxycarbonyl, (CH₂)_(n) -phenyl, C₆₋₁₀ aryloxy, C₆₋₁₀ aryloxycarbonyl, C₆₋₁₀ arylmethylcarbonyl, C₁₋₄ alkylcarbonyloxy C₁₋₄ alkoxycarbonyl, C₆₋₁₀ arylcarbonyloxy C₁₋₄ alkoxycarbonyl, C₁₋₆ alkylaminocarbonyl, phenylaminocarbonyl, and phenyl-C₁₋₄ alkoxycarbonyl;

R⁸, at each occurrence, is selected from H, C₁₋₆ alkyl and (CH₂)_(n) -phenyl;

alternatively, R⁷ and R⁸ combine to form a 5 or 6 membered saturated, ring which contains from 0-1 additional heteroatoms selected from the group consisting of N, O, and S;

R⁹, at each occurrence, is selected from H, C₁₋₆ alkyl and (CH₂)_(n) -phenyl;

n is selected from 0, 1, 2, and 3;

m is selected from 0, 1, and 2;

p is selected from 0, 1, and 2;

r is selected from 0, 1, 2, and 3;

s is selected from 0, 1, and 2; and,

t is selected from 0 and 1.

[2] In a preferred embodiment, the present invention provides novel compounds of formulae Ia-Io: ##STR6## wherein: Z is selected from a bond, CH₂ O, OCH₂, CH₂ NH, NHCH₂, CH₂ C(O), C(O)CH₂, C(O)NH, C(O)NH, CH₂ S(O)₂, S(O)₂ (CH₂), SO₂ NH, and SO₂ NH;

B is selected from: Y, X--Y, and NR² R^(2a) ;

Y is selected from one of the following carbocyclic and heterocyclic systems which are substituted with 0-2 R^(4a) ;

phenyl, piperidinyl, piperazinyl, pyridyl, pyrimidyl, furanyl, morpholinyl, thiophenyl, pyrrolyl, pyrrolidinyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, oxadiazole, thiadiazole, triazole, 1,2,3-oxadiazole, 1,2,4-oxadiazole, 1,2,5-oxadiazole, 1,3,4-oxadiazole, 1,2,3-thiadiazole, 1,2,4-thiadiazole, 1,2,5-thiadiazole, 1,3,4-thiadiazole, 1,2,3-triazole, 1,2,4-triazole, 1,2,5-triazole, 1,3,4-triazole, benzofuran, benzothiofuran, indole, benzimidazole, benzoxazole, benzthiazole, indazole, benzisoxazole, benzisothiazole, and isoindazole;

Y may also be selected from the following bicyclic heteroaryl ring systems: ##STR7## K is selected from O, S, NH, and N.

[3] In a more preferred embodiment, the present invention provides novel compounds of formulae: ##STR8## wherein D is selected from C(═NR⁷)NR⁸ R⁹ and; (CR⁸ R⁹)_(t) NR⁸ R⁹ ;

R is selected from H, F, Cl, OR³, CH₂ OR³, CH₂ NH₂ ;

A is selected from:

piperidinyl,

piperazinyl,

C₅₋₆ carbocyclic residue substituted with 0-2 R⁴, and

5-6 membered heteroaryl containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R⁴ ;

Y is selected from one of the following carbocyclic and heterocyclic systems which are substituted with 0-2 R^(4a) ;

phenyl, piperidinyl, piperazinyl, pyridyl, pyrimidyl, furanyl, morpholinyl, thiophenyl, pyrrolyl, pyrrolidinyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, benzimidazolyl, oxadiazole, thiadiazole, triazole, 1,2,3-oxadiazole, 1,2,4-oxadiazole, 1,2,5-oxadiazole, 1,3,4-oxadiazole, 1,2,3-thiadiazole, 1,2,4-thiadiazole, 1,2,5-thiadiazole, 1,3,4-thiadiazole, 1,2,3-triazole, 1,2,4-triazole, 1,2,5-triazole, and 1,3,4-triazole.

[4] In an even more preferred embodiment, the present invention provides novel compounds wherein:

E is phenyl;

D is selected from C(═NH)NH₂ and CH₂ NH₂ ;

R is selected from H, F, Cl, and Br;

A is selected from:

C₅₋₆ carbocyclic residue substituted with 0-2 R⁴, and

5-6 membered heteroaryl containing from 1-3 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R⁴ ;

Y is selected from one of the following carbocyclic and heterocyclic systems which are substituted with 0-2 R^(4a) ;

phenyl, piperidinyl, piperazinyl, pyridyl, pyrimidyl, furanyl, morpholinyl, thiophenyl, pyrrolyl, pyrrolidinyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, benzimidazolyl, oxadiazole, thiadiazole, triazole, 1,2,3-oxadiazole, 1,2,4-oxadiazole, 1,2,5-oxadiazole, 1,3,4-oxadiazole, 1,2,3-thiadiazole, 1,2,4-thiadiazole, 1,2,5-thiadiazole, 1,3,4-thiadiazole, 1,2,3-triazole, 1,2,4-triazole, 1,2,5-triazole, and 1,3,4-triazole;

R², at each occurrence, is selected from H, CF₃, C₁₋₆ alkyl, benzyl, C₅₋₆ carbocyclic residue substituted with 0-2 R^(4b), and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R^(4b) ;

R^(2a), at each occurrence, is selected from H, CF₃, C₁₋₆ alkyl, benzyl, phenethyl, C₅₋₆ carbocyclic residue substituted with 0-2 R^(4b), and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R^(4b) ;

R^(2b), at each occurrence, is selected from CF₃, C₁₋₄ alkoxy, C₁₋₆ alkyl, benzyl, C₅₋₆ carbocyclic residue substituted with 0-2 R^(4b), and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R^(4b) ;

R^(2c), at each occurrence, is selected from CF₃, OH, C₁₋₄ alkoxy, C₁₋₆ alkyl, benzyl, C₅₋₆ carbocyclic residue substituted with 0-2 R^(4b), and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R^(4b) ;

alternatively, R² and R^(2a), together with the atom to which they are attached, combine to form a ring selected from imidazolyl, morpholino, piperazinyl, pyridyl, and pyrrolidinyl, substituted with 0-2 R^(4b) ;

R⁴, at each occurrence, is selected from H, ═O, OR², CH₂ OR², F, Cl, C₁₋₄ alkyl, NR² R^(2a), CH₂ NR² R^(2a), C(O)R^(2c), CH₂ C(O)R^(2c), C(O)NR² R^(2a), CH(═NR²)NR² R^(2a), CH(═NS(O)₂ R⁵)NR² R^(2a), SO₂ NR² R^(2a), NR² SO₂ -C₁₋₄ alkyl, S(O)₂ R⁵, and CF₃ provided that if B is H, then R⁴ is other than tetrazole, C(O)-alkoxy, and C(O)NR² R^(2a) ;

R^(4a), at each occurrence, is selected from H, ═O, (CH₂)_(r) OR², F, Cl, C₁₋₄ alkyl, NR² R^(2a), CH₂ NR² R^(2a), NR² R^(2b), CH₂ NR² R^(2b), (CH₂)_(r) C(O)R^(2c), NR² C(O)R^(2b), C(O)NR² R^(2a), C(O)NH(CH₂)₂ NR² R^(2a), NR² C(O)NR² R^(2a), SO₂ NR² R^(2a), S(O)₂ R⁵, and CF₃ ; and,

R^(4b), at each occurrence, is selected from H, ═O, (CH₂)_(r) OR³, F, Cl, C₁₋₄ alkyl, NR³ R^(3a), CH₂ NR³ R^(3a), C(O)R³, CH₂ C(O)R³, C(O)OR^(3c), C(O)NR³ R^(3a), CH(═NR³)NR³ R^(3a), SO₂ NR³ R^(3a), NR³ SO₂ -C₁₋₄ alkyl, NR³ SO₂ CF₃, NR³ SO₂ -phenyl, S(O)₂ CF₃, S(O)₂ -C₁₋₄ alkyl, S(O)₂ -phenyl, and CF₃.

[5] In a further preferred embodiment, the present invention provides novel compounds selected from:

N-(2'-Aminosulfonyl-[1,1']biphen-4-yl)-2-(3'-amidinophenyl)nicotinamide;

N-[5-(2-aminosulfonyl)phenylpyrid-2-yl]-2-(3'-amidinophenyl)nicotinamide;

N-[5-(2-t-butylaminosulfonyl)phenylpyrid-2-yl]-2-(3'-amidinophenyl)nicotinamide; and,

N-[5-(2-aminosulfonyl)phenylpyrid-2-yl]-2-(3'-carboxamidophenyl)nicotinamide;

or a pharmaceutically acceptable salt thereof.

In a second embodiment, the present invention provides novel pharmaceutical compositions, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt form thereof.

In a third embodiment, the present invention provides a novel method for treating or preventing a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt form thereof.

DEFINITIONS

The compounds herein described may have asymmetric centers. Compounds of the present invention containing an asymmetrically substituted atom may be isolated in optically active or racemic forms. It is well known in the art how to prepare optically active forms, such as by resolution of racemic forms or by synthesis from optically active starting materials. Many geometric isomers of olefins, C═N double bonds, and the like can also be present in the compounds described herein, and all such stable isomers are contemplated in the present invention. Cis and trans geometric isomers of the compounds of the present invention are described and may be isolated as a mixture of isomers or as separated isomeric forms. All chiral, diastereomeric, racemic forms and all geometric isomeric forms of a structure are intended, unless the specific stereochemistry or isomeric form is specifically indicated.

The term "substituted," as used herein, means that any one or more hydrogens on the designated atom is replaced with a selection from the indicated group, provided that the designated atom's normal valency is not exceeded, and that the substitution results in a stable compound. When a substitent is keto (i.e., ═O), then 2 hydrogens on the atom are replaced. Keto substituents are not present on aromatic moieties.

The present invention is intended to include all isotopes of atoms occurring in the present compounds. Isotopes include those atoms having the same atomic number but different mass numbers. By way of general example and without limitation, isotopes of hydrogen include tritium and deuterium. Isotopes of carbon include C-13 and C-14.

When any variable (e.g., R⁶) occurs more than one time in any constituent or formula for a compound, its definition at each occurrence is independent of its definition at every other occurrence. Thus, for example, if a group is shown to be substituted with 0-2 R⁶, then said group may optionally be substituted with up to two R⁶ groups and R⁶ at each occurrence is selected independently from the definition of R⁶. Also, combinations of substituents and/or variables are permissible only if such combinations result in stable compounds.

When a bond to a substituent is shown to cross a bond connecting two atoms in a ring, then such substituent may be bonded to any atom on the ring. When a substituent is listed without indicating the atom via which such substituent is bonded to the rest of the compound of a given formula, then such substituent may be bonded via any atom in such substituent. Combinations of substituents and/or variables are permissible only if such combinations result in stable compounds.

As used herein, "alkyl" is intended to include both branched and straight-chain saturated aliphatic hydrocarbon groups having the specified number of carbon atoms. Examples of alkyl include, but are not limited to, methyl, ethyl, n-propyl, i-propyl, n-butyl, s-butyl, t-butyl, n-pentyl, and s-pentyl. "Haloalkyl" is intended to include both branched and straight-chain saturated aliphatic hydrocarbon groups having the specified number of carbon atoms, substituted with 1 or more halogen (for example --C_(v) F_(w) where v=1 to 3 and w=1 to (2v+1)). Examples of haloalkyl include, but are not limited to, trifluoromethyl, trichloromethyl, pentafluoroethyl, and pentachloroethyl. "Alkoxy" represents an alkyl group as defined above with the indicated number of carbon atoms attached through an oxygen bridge. Examples of alkoxy include, but are not limited to, methoxy, ethoxy, n-propoxy, i-propoxy, n-butoxy, s-butoxy, t-butoxy, n-pentoxy, and s-pentoxy. "Cycloalkyl" is intended to include saturated ring groups, such as cyclopropyl, cyclobutyl, or cyclopentyl. Alkenyl" is intended to include hydrocarbon chains of either a straight or branched configuration and one or more unsaturated carbon-carbon bonds which may occur in any stable point along the chain, such as ethenyl, propenyl and the like. "Alkynyl" is intended to include hydrocarbon chains of either a straight or branched configuration and one or more triple carbon-carbon bonds which may occur in any stable point along the chain, such as ethynyl, propynyl and the like.

"Halo" or "halogen" as used herein refers to fluoro, chloro, bromo, and iodo; and "counterion" is used to represent a small, negatively charged species such as chloride, bromide, hydroxide, acetate, sulfate, and the like.

As used herein, "carbocycle" or "carbocyclic residue" is intended to mean any stable 3- to 7-membered monocyclic or bicyclic or 7- to 13-membered bicyclic or tricyclic, any of which may be saturated, partially unsaturated, or aromatic. Examples of such carbocycles include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, adamantyl, cyclooctyl, [3.3.0]bicyclooctane, [4.3.0]bicyclononane, [4.4.0]bicyclodecane, [2.2.2]bicyclooctane, fluorenyl, phenyl, naphthyl, indanyl, adamantyl, or tetrahydronaphthyl.

As used herein, the term "heterocycle" or "heterocyclic system" is intended to mean a stable 5- to 7-membered monocyclic or bicyclic or 7- to 10-membered bicyclic heterocyclic ring which is saturated partially unsaturated or unsaturated (aromatic), and which consists of carbon atoms and from 1 to 4 heteroatoms independently selected from the group consisting of N, O and S and including any bicyclic group in which any of the above-defined heterocyclic rings is fused to a benzene ring. The nitrogen and sulfur heteroatoms may optionally be oxidized. The heterocyclic ring may be attached to its pendant group at any heteroatom or carbon atom which results in a stable structure. The heterocyclic rings described herein may be substituted on carbon or on a nitrogen atom if the resulting compound is stable. If specifically noted, a nitrogen in the heterocycle may optionally be quaternized. It is preferred that when the total number of S and O atoms in the heterocycle exceeds 1, then these heteroatoms are not adjacent to one another. It is preferred that the total number of S and O atoms in the heterocycle is not more than 1. As used herein, the term "aromatic heterocyclic system" is intended to mean a stable 5- to 7-membered monocyclic or bicyclic or 7- to 10-membered bicyclic heterocyclic aromatic ring which consists of carbon atoms and from 1 to 4 heterotams independently selected from the group consisting of N, O and S. It is preferred that the total number of S and O atoms in the aromatic heterocycle is not more than 1.

Examples of heterocycles include, but are not limited to, acridinyl, azocinyl, benzimidazolyl, benzofuranyl, benzothiofuranyl, benzothiophenyl, benzoxazolyl, benzthiazolyl, benztriazolyl, benztetrazolyl, benzisoxazolyl, benzisothiazolyl, benzimidazolinyl, carbazolyl, 4aH-carbazolyl, carbolinyl, chromanyl, chromenyl, cinnolinyl, decahydroquinolinyl, 2H,6H-1,5,2-dithiazinyl, dihydrofuro[2,3-b]tetrahydrofuran, furanyl, furazanyl, imidazolidinyl, imidazolinyl, imidazolyl, 1H-indazolyl, indolenyl, indolinyl, indolizinyl, indolyl, 3H-indolyl, isobenzofuranyl, isochromanyl, isoindazolyl, isoindolinyl, isoindolyl, isoquinolinyl, isothiazolyl, isoxazolyl, morpholinyl, naphthyridinyl, octahydroisoquinolinyl, oxadiazolyl, 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,5-oxadiazolyl, 1,3,4-oxadiazolyl, oxazolidinyl, oxazolyl, oxazolidinyl, pyrimidinyl, phenanthridinyl, phenanthrolinyl, phenazinyl, phenothiazinyl, phenoxathiinyl, phenoxazinyl, phthalazinyl, piperazinyl, piperidinyl, pteridinyl, purinyl, pyranyl, pyrazinyl, pyrazolidinyl, pyrazolinyl, pyrazolyl, pyridazinyl, pyridooxazole, pyridoimidazole, pyridothiazole, pyridinyl, pyridyl, pyrimidinyl, pyrrolidinyl, pyrrolinyl, 2H-pyrrolyl, pyrrolyl, quinazolinyl, quinolinyl, 4H-quinolizinyl, quinoxalinyl, quinuclidinyl, tetrahydrofuranyl, tetrahydroisoquinolinyl, tetrahydroquinolinyl, 6H-1,2,5-thiadiazinyl, 1,2,3-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,5-thiadiazolyl, 1,3,4-thiadiazolyl, thianthrenyl, thiazolyl, thienyl, thienothiazolyl, thienooxazolyl, thienoimidazolyl, thiophenyl, triazinyl, 1,2,3-triazolyl, 1,2,4-triazolyl, 1,2,5-triazolyl, 1,3,4-triazolyl, and xanthenyl. Preferred heterocycles include, but are not limited to, pyridinyl, furanyl, thienyl, pyrrolyl, pyrazolyl, pyrrolidinyl, imidazolyl, indolyl, benzimidazolyl, 1H-indazolyl, oxazolidinyl, benzotriazolyl, benzisoxazolyl, oxindolyl, benzoxazolinyl, or isatinoyl. Also included are fused ring and Spiro compounds containing, for example, the above heterocycles.

The phrase "pharmaceutically acceptable" is employed herein to refer to those compounds, materials, compositions, and/or dosage forms which are, within the scope of sound medical judgment, suitable for use in contact with the tissues of human beings and animals without excessive toxicity, irritation, allergic response, or other problem or complication, commensurate with a reasonable benefit/risk ratio.

As used herein, "pharmaceutically acceptable salts" refer to derivatives of the disclosed compounds wherein the parent compound is modified by making acid or base salts thereof. Examples of pharmaceutically acceptable salts include, but are not limited to, mineral or organic acid salts of basic residues such as amines; alkali or organic salts of acidic residues such as carboxylic acids; and the like. The pharmaceutically acceptable salts include the conventional non-toxic salts or the quaternary ammonium salts of the parent compound formed, for example, from non-toxic inorganic or organic acids. For example, such conventional non-toxic salts include those derived from inorganic acids such as hydrochloric, hydrobromic, sulfuric, sulfamic, phosphoric, nitric and the like; and the salts prepared from organic acids such as acetic, propionic, succinic, glycolic, stearic, lactic, malic, tartaric, citric, ascorbic, pamoic, maleic, hydroxymaleic, phenylacetic, glutamic, benzoic, salicylic, sulfanilic, 2-acetoxybenzoic, fumaric, toluenesulfonic, methanesulfonic, ethane disulfonic, oxalic, isethionic, and the like.

The pharmaceutically acceptable salts of the present invention can be synthesized from the parent compound which contains a basic or acidic moiety by conventional chemical methods. Generally, such salts can be prepared by reacting the free acid or base forms of these compounds with a stoichiometric amount of the appropriate base or acid in water or in an organic solvent, or in a mixture of the two; generally, nonaqueous media like ether, ethyl acetate, ethanol, isopropanol, or acetonitrile are preferred. Lists of suitable salts are found in Remington's Pharmaceutical Sciences, 17th ed., Mack Publishing Company, Easton, Pa., 1985, p. 1418, the disclosure of which is hereby incorporated by reference.

"Prodrugs" are intended to include any covalently bonded carriers which release the active parent drug according to formula (I) in vivo when such prodrug is administered to a mammalian subject. Prodrugs of a compound of formula (I) are prepared by modifying functional groups present in the compound in such a way that the modifications are cleaved, either in routine manipulation or in vivo, to the parent compound. Prodrugs include compounds of formula (I) wherein a hydroxy, amino, or sulfhydryl group is bonded to any group that, when the prodrug or compound of formula (I) is administered to a mammalian subject, cleaves to form a free hydroxyl, free amino, or free sulfhydryl group, respectively. Examples of prodrugs include, but are not limited to, acetate, formate and benzoate derivatives of alcohol and amine functional groups in the compounds of formula (I), and the like. Preferred prodrugs are amidine prodrugs wherein D is C(═NR⁷)NH₂, and R⁷ is selected from OH, C₁₋₄ alkoxy, C₆₋₁₀ aryloxy, C₁₋₄ alkoxycarbonyl, C₆₋₁₀ aryloxycarbonyl, C₆₋₁₀ arylmethylcarbonyl, C₁₋₄ alkylcarbonyloxy C₁₋₄ alkoxycarbonyl, and C₆₋₁₀ arylcarbonyloxy C₁₋₄ alkoxycarbonyl. More preferred prodrugs are where R⁷ is OH, methoxy, ethoxy, benzyloxycarbonyl, methoxycarbonyl, and methylcarbonyloxymethoxycarbonyl.

"Stable compound" and "stable structure" are meant to indicate a compound that is sufficiently robust to survive isolation to a useful degree of purity from a reaction mixture, and formulation into an efficacious therapeutic agent.

"Substituted" is intended to indicate that one or more hydrogens on the atom indicated in the expression using "substituted" is replaced with a selection from the indicated group(s), provided that the indicated atom's normal valency is not exceeded, and that the substitution results in a stable compound. When a substituent is keto (i.e., ═O) group, then 2 hydrogens on the atom are replaced.

"Therapeutically effective amount" is intended to include an amount of a compound of the present invention or an amount of the combination of compounds claimed effective to inhibit HIV infection or treat the symptoms of HIV infection in a host. The combination of compounds is preferably a synergistic combination. Synergy, as described for example by Chou and Talalay, Adv. Enzyme Regul. 22:27-55 (1984), occurs when the effect (in this case, inhibition of HIV replication) of the compounds when administered in combination is greater than the additive effect of the compounds when administered alone as a single agent. In general, a synergistic effect is most clearly demonstrated at suboptimal concentrations of the compounds. Synergy can be in terms of lower cytotoxicity, increased antiviral effect, or some other beneficial effect of the combination compared with the individual components.

SYNTHESIS

The compounds of the present invention can be prepared in a number of ways known to one skilled in the art of organic synthesis. The compounds of the present invention can be synthesized using the methods described below, together with synthetic methods known in the art of synthetic organic chemistry, or variations thereon as appreciated by those skilled in the art. Preferred methods include, but are not limited to, those described below. The reactions are performed in a solvent appropriate to the reagents and materials employed and suitable for the transformations being effected. It will sometimes require a judgment to modify the order of synthetic steps or to select one particular process scheme over another in order to obtain a desired compound of the invention. It will also be recognized that another major consideration in the planning of any synthetic route in this field is the judicious choice of the protecting group used for the protection of the reactive functional groups present in the compounds described in this invention. An authoritative account describing the many alternatives to the trained practitioner is Greene and Wuts (Protective Groups in Organic Chemistry, Wiley and Sons, 1991). All references cited herein are hereby incorporated in their entirety herein by reference. Compounds of this invention where B is either a carbocyclic or heterocyclic residue as defined in Formula 1 are coupled to A as shown generically and by specific example in Schemes 1 and 2, respectively. Either or both of A and B may be substituted with 0-2 R⁴. W is defined as a suitable protected nitrogen, such as NO₂ or NHBOC; a protected sulfur, such as S-tBu or SMOM; or a methyl ester. Halogen-metal exchange of the bromine in bromo-B with n-butyl lithium, quenching with triisopropyl borate and acidic hydrolysis gives the required boronic acid, B--B(OH)₂. The W--A--Br subunit may be already linked to ring M before the Suzuki coupling reaction. Deprotection provides the complete subunit. ##STR9##

Scheme 2 describes a typical example of how the A-B subunit is prepared for attachment to ring M. 4-Bromoaniline is protected as Boc-derivative and the coupled to 2-(t-butylamino)sulfonylphenylboronic acid under Suzuki conditions. 2-(t-Butylamino)sulfonylphenylboronic acid is prepared by the method described by Rivero (Bioorg. Med. Chem. Lett. 1994, 189). Deprotection with TFA can provide the aminobiphenyl compound. The aminobiphenyl is then coupled to the core ring structures as described below. ##STR10##

When B is defined as X--Y, the following description applies. Groups A and B are available either through commercial sources, known in the literature or readily synthesized by the adaptation of standard procedures known to practitioners skilled in the art of organic synthesis. the required reactive functional groups appended to analogs of A and B are also available either through commercial sources, known in the literature or readily synthesized by the adaptation of standard procedures known to practitioners skilled in the art of synthesis. In the tables that follow the chemistry required to effect the coupling of A to B is outlined.

                  TABLE A                                                          ______________________________________                                         Preparation of Amide Ester, Urea, Sulfonamide and                                Sulfamide Linkages Between A and B.                                                         then the reactive                                                                           to give the following                                If A contains: substituent of Y is: product A--X--Y:                         ______________________________________                                         A--NHR.sup.2 as a                                                                         ClC(O)--Y    A--NR.sup.2 --C(O)--Y                                    substituent                                                                    a secondary NH ClC(O)--Y A--C(O)--Y                                            as part of a                                                                   ring or chain                                                                  A--OH as a ClC(O)--Y A--O--C(O)--Y                                             substituent                                                                    A--NHR.sup.2 as a ClC(O)--CR.sup.2 R.sup.2a -- A--NR.sup.2 --C(O)--CR.su                             p.2 R.sup.2a --Y                                         substituent --Y                                                                a secondary NH ClC(O)--CR.sup.2 R.sup.2a -- A--C(O)--CR.sup.2 R.sup.2a                               --Y                                                      as part of a --Y                                                               ring or chain                                                                  A--OH as a ClC(O)--CR.sup.2 R.sup.2a -- A--O--C(O)--CR.sup.2 R.sup.2a                                --Y                                                      substituent --Y                                                                A--NHR.sup.2 as a ClC(O)--CNR.sup.2 --Y A--NR.sup.2 --C(O)--CNR.sup.2                                --Y                                                      substituent                                                                    a secondary NH ClC(O)--CNR.sup.2 --Y A--C(O)--CNR.sup.2 --Y                    as part of a                                                                   ring or chain                                                                  A--OH as a ClC(O)--CNR.sup.2 --Y A--O--C(O)--CNR.sup.2 --Y                     substituent                                                                    A--NHR.sup.2 as a ClSO.sub.2 --Y A--NR.sup.2 --SO.sub.2 --Y                    substituent                                                                    a secondary NH ClSO.sub.2 --Y A--SO.sub.2 --Y                                  as part of a                                                                   ring or chain                                                                  A--NHR.sup.2 as a ClSO.sub.2 --CR.sup.2 R.sup.2a -- A--NR.sup.2                                      --SO.sub.2 --CR.sup.2 R.sup.2a --Y                       substituent --Y                                                                a secondary NH ClSO.sub.2 --CR.sup.2 R.sup.2a -- A--SO.sub.2 --CR.sup.2                              R.sup.2a --Y                                             as part of a --Y                                                               ring or chain                                                                  A--NHR.sup.2 as a ClSO.sub.2 --NR.sup.2 --Y A--NR.sup.2 --SO.sub.2                                   --NR.sup.2 --Y                                           substituent                                                                    a secondary NH ClSO.sub.2 --NR.sup.2 --Y A--SO.sub.2 --NR.sup.2 --Y                                   as part of a                                            ring or chain                                                                  A--C(O)Cl HO--Y as a A--C(O)--O--Y                                              substituent                                                                   A--C(O)Cl NHR.sup.2 --Y as a A--C(O)--NR.sup.2 --Y                              substituent                                                                   A--C(O)Cl a secondary NH as A--C(O)--Y                                          part of a ring or                                                              chain                                                                         A--CR.sup.2 R.sup.2a C(O)Cl HO--Y as a A--CR.sup.2 R.sup.2a C(O)--O--Y                                 substituent                                            A--CR.sup.2 R.sup.2a C(O)Cl NHR.sup.2 --Y as a A--CR.sup.2 R.sup.2a                                  C(O)--NR.sup.2 --Y                                        substituent                                                                   A--CR.sup.2 R.sup.2a C(O)Cl a secondary NH as A--CR.sup.2 R.sup.2a                                   C(O)--Y                                                   part of a ring or                                                              chain                                                                         A--SO.sub.2 Cl NHR.sup.2 --Y as a A--SO.sub.2 --NR.sup.2 --Y                    substituent                                                                   A--SO.sub.2 Cl a secondary NH as A--SO.sub.2 --Y                                part of a ring or                                                              chain                                                                         A--CR.sup.2 R.sup.2a SO.sub.2 Cl NHR.sup.2 --Y as a A--CR.sup.2                                      R.sup.2a SO.sub.2 --NR.sup.2 --Y                          substituent                                                                   A--CR.sup.2 R.sup.2a SO.sub.2 Cl a secondary NH as A--CR.sup.2 R.sup.2a                              SO.sub.2 --Y                                              part of a ring or                                                              chain                                                                       ______________________________________                                    

The chemistry of Table A can be carried out in aprotic solvents such as a chlorocarbon, pyridine, benzene or toluene, at temperatures ranging from -20° C. to the reflux point of the solvent and with or without a trialkylamine base.

                  TABLE B                                                          ______________________________________                                         Preparation of Ketone Linkages between A and B.                                               then the reactive                                                                           to give the following                                If A contains: substituent of Y is: product A--X--Y:                         ______________________________________                                         A--C(O)Cl  BrMg--Y      A--C(O)--Y                                               A--CR.sup.2 R.sup.2a C(O)Cl BrMg--Y A--CR.sup.2 R.sup.2a C(O)--Y                                      A--C(O)Cl BrMgCR.sup.2 R.sup.2a --Y A--C(O)CR.sup                             .2 R.sup.2a --Y                                          A--CR.sup.2 R.sup.2a C(O)Cl BrMgCR.sup.2 R.sup.2a --Y A--CR.sup.2                                    R.sup.2a C(O)CR.sup.2 R.sup.2a --Y                     ______________________________________                                    

The coupling chemistry of table B can be carried out by a variety of methods. The Grignard reagent required for Y is prepared from a halogen analog of Y in dry ether, dimethoxyethane or tetrahydrofuran at 0° C. to the reflux point of the solvent. This Grignard reagent can reacted directly under very controlled conditions, that is low temperature (-20° C. or lower) and with a large excess of acid chloride or with catalytic or stoichiometric copper bromide•dimethyl sulfide complex in dimethyl sulfide as a solvent or with a variant thereof. Other methods available include transforming the Grignard reagent to the cadmium reagent and coupling according to the procedure of Carson and Prout (Org. Syn. Col. Vol. 3 (1955) 601) or a coupling mediated by Fe(acac)3 according to Fiandanese et al. (Tetr. Lett. 1984, 4805), or a coupling mediated by manganese (II) catalysis (Cahiez and Laboue, Tetr. Lett. 1992, 33(31), 4437).

                  TABLE C                                                          ______________________________________                                         Preparation of Ether and Thioether linkages between                              A and B.                                                                                      then the reactive                                                                            to give the following                             If A contains: substituent of Y is: product A--X--Y:                         ______________________________________                                         A--OH        Br--Y         A--O--Y                                               A--CR.sup.2 R.sup.2a --OH Br--Y A--CR.sup.2 R.sup.2a O--Y                      A--OH Br--CR.sup.2 R.sup.2a --Y A--OCR.sup.2 R.sup.2a --Y                      A--SH Br--Y A--S--Y                                                            A--CR.sup.2 R.sup.2a --SH Br--Y A--CR.sup.2 R.sup.2a S--Y                      A--SH Br--CR.sup.2 R.sup.2a --Y A--SCR.sup.2 R.sup.2a --Y                    ______________________________________                                    

The ether and thioether linkages of Table C can be prepared by reacting the two components in a polar aprotic solvent such as acetone, dimethylformamide or dimethylsulfoxide in the presence of a base such as potassium carbonate, sodium hydride or potassium t-butoxide at a temperature ranging from ambient to the reflux point of the solvent used.

                  TABLE D                                                          ______________________________________                                         Preparation of --SO-- and --SO.sub.2 -- linkages from                            thioether of Table C.                                                                       then it is oxidized                                                                           then it is oxidized                                 with wet with m-                                                              If the starting Alumina/Oxone to chloroperbenzoic acid                         material is: give: to give:                                                  ______________________________________                                         A--S--Y    A--S(O)--Y     A--SO.sub.2 --Y                                        A--CR.sup.2 R.sup.2a S--Y A--CR.sup.2 R.sup.2a S(O)--Y A--CR.sup.2                                     R.sup.2a SO.sub.2 --Y                                  A--SCR.sup.2 R.sup.2a --Y A--S(O)CR.sup.2 R.sup.2a --Y A--SO.sub.2                                     CR.sup.2 R.sup.2a --Y                                ______________________________________                                    

The thioethers of Table C serve as a convenient starting material for the preparation of the sulfoxide and sulfone analogs of Table D. A combination of wet alumina and Oxone can provide a reliable reagents for the oxidation of the thioether to the sulfoxide as shown by Greenhalgh (Syn. Lett. 1992, 235). The sulfone can be prepared according to the method of Satoh (Chem. Lett. 1992, 381) using m-chloroperbenzoic acid.

Scheme 3 describes the synthesis of compounds wherein M is a benzene ring and Q is a protected precursor of group D of Formula I and V is a nitro, protected sulfonamide or ester group and precursor of group Z of Formula I. The V group is placed on an appropriately substituted phenol either via nitration as shown by Poirier et al. (Tetrahedron 1989, 45(5), 1415), sulfonylation as shown by Kuznetsov (Akad. Nauk SSSR Ser. Khim 1990, 8, 1888) or carboxylation by Sartori et al. (Synthesis 1988, 10, 763). Bromination with triphenylphosphine and bromine (J. Am. Chem. Soc. 1964, 86, 964) gives the desired bromide. Suzuki coupling with the appropriate boronic acid provides the desired substituted pyridine. ##STR11##

Schemes 4, 5, 6, and 7 describe the synthesis of compounds wherein M is pyridine and Q is a protected precursor of group D of Formula I. Each scheme represents a different substitution pattern for the pyridine ring. In Scheme 4, a suitably protected aldehyde is subjected to base-catalyzed condensation with an activated ester to give after deprotection the desired aldehyde. Refluxing with ammonium chloride as shown by Dornow and Ische (Chem. Ber. 1956, 89, 876) provides the pyridinol which is brominated with POBr₃ (Tjeenk et al. Rec. Trav. Chim. 1948, 67, 380) to give the desired 2-bromopyridine. Suzuki coupling with the appropriate boronic acid provides the desired substituted pyridine. ##STR12##

Treatment of an appropriately substituted 5-ethoxyoxazole with an alkene as shown by Kondrat'eva et al. Dokl. Akad. Nauk SSSR 1965, 164, 816) provides a pyridine with the V substituent at the para position. Bromination at the 3-position as shown by van der Does and Hertog (Rec. Trav. Khim. Pays-Bas 1965, 84, 951) followed by palladium-catalyzed boronic acid coupling provides the desired substituted pyridine. ##STR13##

Scheme 6 describes a synthesis of a third substitution pattern on a pyridine ring. The appropriate tricarbonyl compound which can be prepared by methods described in Scheme 4 is treated with ammonium chloride to form the pyridinol which is subsequently brominated. Palladium-catalyzed coupling provides the desired substituted pyridine. ##STR14##

Scheme 7 takes a suitably substituted dicarbonyl compound and by chemistry illustrated in Schemes 4 and 6, reacts it with ammonium chloride. Bromination gives the 3-bromopyridine which upon palladium-catalyzed coupling provides the desired substituted pyridine. ##STR15##

Schemes 8, 9, and 10 describe the synthesis of compounds wherein M is pyridazine and Q is a protected precursor of group D of Formula I. Each scheme represents a different substitution pattern for the pyridine ring. In Scheme 8 an activated ester is reacted with an appropriately substituted α-keto aldehyde and hydrazine as shown by Schmidt and Druey (Helv. Chim. Acta 1954, 37, 134 and 1467). Conversion of the pyridazinone to the bromide using POBr₃ and palladium-catalized coupling provides the desired substituted pyridazine. ##STR16##

In Scheme 9, glyoxal can react under basic conditions with an activated ketone and subsequently brominated/dehydro-brominated to give the desired ketoaldehyde. Alternatively, a protected ketone can react with an activated aldehyde, undergo bromination/dehydrobromination, be deprotected and oxidized to give the regioisomeric ketoaldehyde. Cyclization as shown by Sprio and Madonia (Ann. Chim. 1958, 48, 1316) with hydrazine followed by palladium-catalyzed coupling provides the desired substituted pyridazine. ##STR17##

By analogy to Scheme 9, in Scheme 10 a aldehyde can be reacted with an activated ketone, brominated, dehydro-brominated and deprotected to give the desired diketone. Alternatively, a regioisomeric ketone can be placed through the same reaction sequence to produce an isomeric keto aldehyde. Reaction with hydrazine followed by palladium-catalized coupling provides the desired substituted pyridazine. ##STR18##

Schemes 11, and 12 describe the synthesis of compounds wherein M is pyrimidine and Q is a protected precursor of group D of Formula I. Each scheme represents a different substitution pattern for the pyrimidine ring. In Scheme 11, a condensation with an appropriately substituted acid chloride and an activated ester followed by conjugate reduction by tin hydride (Moriya et al. J. Org. Chem. 1986, 51, 4708) gives the desired 1,4 dicarbonyl compound. Cyclization with formamidine or a substituted amidine followed by bromination gives the desired regioisomeric pyrimidine. Palladium-catalyzed coupling provides the desired substituted pyrimidine. ##STR19##

Using similar chemistry, Scheme 12 shows how an amidine can be condensed with a 1,3-dicarbonyl compound and subsequently brominated in the 5-position (J. Het. Chem. 1973, 10, 153) to give a specific regioisomeric bromopyrimidine. Palladium-catalyzed coupling provides the desired substituted pyrimidine. ##STR20##

Using the same ketoaldehyde from Scheme 12, cyclization with an appropriately substituted 1,2-diamine (Chimia 1967, 21, 510) followed by aromatization (Helv. Chim. Acta 1967, 50, 1754) provides a regioisomeric mixture of pyrazines as illustrated in Scheme 13. Bromination of the hydrobromide salt (U.S. Pat. No. 2,403,710) yields the intermediate for the palladium-catalyzed coupling step which occurs as shown above. ##STR21##

Schemes 14 and 15 describe the synthesis of compounds wherein M is a 1,2,3-triazine and Q is a protected precursor of group D of Formula I. In Scheme 14, a vinyl bromide is palladium coupled to a molecule containing the substituent R^(1b). Allylic bromination followed by azide displacement provide the cyclization precursor. Triphenylphosphine-mediated cyclization (J. Org. Chem. 1990, 55, 4724) give the 1-aminopyrazole which is subsequently brominated with N-bromosuccimide. Lead tetraacetate mediated rearrangement as shown by Neunhoeffer et al. (Ann. 1985, 1732) provides the desired regioisomeric 1,2,3-triazine. Palladium-catalyzed coupling provides the substituted triazine. ##STR22##

In Scheme 15, an alkene is allylically brominated and the bromide is displaced to give a regioisomer of the azide in Scheme 14. Following the same reaction sequence as shown above, cyclization provides the 1-aminopyrazole. Bromination followed by lead tetraacetate mediated rearrangement give the 1,2,3-triazine. Palladium-catalyzed coupling provides the other desired triazine. ##STR23##

Schemes 16 and 17 describe the synthesis of compounds wherein M is a 1,2,4-triazine and Q is a protected precursor of group D of Formula I. In Scheme 16, a nitrile is converted using hydrazine to give the amidrazone which is condensed with a α-ketoester to give the triazinone as shown by Paudler and Lee (J. Org. Chem. 1971, 36, 3921). Bromination as shown by Rykowski and van der Plas (J. Org. Chem. 1987, 52, 71) followed by palladium-catalyzed coupling provides the desired 1,2,4-triazine. ##STR24##

In Scheme 16, to achieve the opposite regioisomer the reaction scheme shown above is modify by the substituting a protect α-ketoester. This allows the most nucleophilic nitrogen to attack the ester functionality setting up the opposite regiochemistry. Deprotection and thermal cyclization gives the triazinone which is brominated as shown above. Palladium-catalyzed coupling provides the other desired 1,2,4-triazine. ##STR25##

Scheme 18 describes the synthesis of compounds wherein M is a 1,2,3,4-tetrazine and Q is a protected precursor of group D of Formula I. Lithiation of a vinyl bromide, transmetallation with tin, palladium catalyzed carbonylation and hydrazone formation provides a diene for a subsequent Diels-Alder reaction as shown by Carboni and Lindsey (J. Am. Chem. Soc. 1959, 81, 4342). Reaction with dibenzyl azodicarboxylate followed by catalytic hydrogenation to debenzylate and decarboxylate should give after bromination the desired 1,2,3,4-tetrazine. Palladium-catalyzed coupling provides the desired substitution. ##STR26##

Other features of the invention will become apparent in the course of the following descriptions of exemplary embodiments which are given for illustration for the invention and are not intended to be limiting thereof.

EXAMPLES Example 1 N-(2'-Aminosulfonyl-[1,1']biphen-4-yl)-2-(3'-amidinophenyl)nicotinamide, trifluoroacetic Acid Salt

Part A. Preparation of 2-bromonicotinic Acid.

Potassium permanganate (18.4 g, 116 mmol) was dissolved in water (400 mL) and added to 2-bromo-3-methylpyridine (10.0 g, 58 mmol) and refluxed for 16 hours. After cooling to room temperature, the slurry was filtered through a celite plug and rinsed with water and chloroform. The entire filtrate was transferred to a separatory funnel and the layers were separated. The aqueous layer was extracted again with CHCl₃ and acidified with 6N HCl to pH 1. A white solid was obtained on standing (2.08 g of product). The pH of the remaining aqueous was adjusted to pH 4 with 2M NaOH and 2M HCl, then concentrated to <100 mL. A white precipitate was filtered. The pH was adjusted to 4 and the mixture filtered again, combining the isolated solids for a total of 3.88 g of product. The filtrate was concentrated again to <100 mL and adjusted to pH 1.5 and an additional quanitity of white solid was obtained (1.80 g), for a combined yield of 3 crops, (8.76 g, 66%). ¹ H NMR (DMSO-d6): δ 13.76 (bs, 1H), 8.46 (m, 1H), 8.09 (dd, 1H, J=7.7, J'=2.2), 7.51 (m, 1H).

Part B. Preparation of methyl 2-bromonicotinate.

2-Bromonicotinic acid (7.33 g, 36 mmol) was suspended in dry Et₂ O (40 mL), and MeOH (2.3 mL) and diethyl azodicarboxylate (5.8 mL, 37 mmol) were added. Triphenylphosphine (9.61 g in 40 mL Et₂ O, 37 mmol) was added dropwise over 2.5 hours. After stirring an additional two hours, the reaction was filtered and evaporated. The resulting clear liquid was chromatographed on silica gel (10-40% EtOAc/hexanes) to yield a clear oil (8.63 g, 100%). ¹ H NMR (CDCl₃): δ 8.49 (dd, 1H, J=4.8, J'=2.2), 8.09 (dd, 1H, J=7.7, J'=1.8), 7.36 (m, 1H), 3.97 (s, 3H).

Part C. Preparation of 3-cyanophenylboronic Acid.

3-Bromobenzonitrile (10.0 g, 55 mmol) was dissolved in dry THF (100 mL) and cooled to -100° C. (Et₂ O/N₂). n-Butyllithium (24.2 mL, 2.5 M in hexane) was added over 30 minutes, maintaining the internal temp under -90°. After 20 minutes, triisopropylborate (18.0 mL) was added over 15 minutes, again maintaining the internal temperature. After the addition was complete, the reaction was allowed to warm slowly to room temperature over 1.5 hours. The reaction was stirred at room temp for 16 hours, then cooled to 15° C., after which 6 M HCl (25 mL) was added. After stirring vigorously for 3.5 hours, the reaction was partitioned between water and EtOAc. After extracting a second time with EtOAc, the combined organics were washed with 2 M NaOH. The aqueous extract was neutralized with 6 M HCl. The white precipitate was filtered, yielding the desired product (4.80 g, 60%). ¹ H NMR (DMSO-d₆): δ 8.37 (s, 2H), 8.10 (s, 1H), 8.03 (dt, 1H, J=7.3, J'=1.1), 7.83 (dt, 1H, J=7.6, J'=1.4), 7.53 (t, 1H, J=7.7).

Part D. Preparation of methyl 2-(3'-cyanophenyl)nicotinate.

Methyl 2-bromonicotinate (2.0 g, 9.3 mmol) and 3-cyanophenylboronic acid (2.7 g, 18.4 mmol) were combined in 190 mL benzene. Sodium carbonate (19 mL of a 2 M aqueous solution), tetrabutylammonium bromide (152 mg, 0.5 mmol), and bis(triphenylphosphine)palladium(II) chloride (325 mg, 0.5 mmol) were added. The entire mixture was evacuated to remove dissolved gasses, then placed under argon. The reaction was refluxed for 14 hours, diluted with water and EtOAc, separated, dried over Na₂ SO₄, filtered, and evaporated. The resulting yellow solid was chromatographed on silica gel (30% EtOAc/hexanes) to yield a light yellow solid (1.70 g, 77%). ¹ H NMR (CDCl₃): δ 8.81 (dd, 1H, J=4.8, J'=1.8), 8.23 (dd, 1H, J=8.0, J'=1.9), 7.85 (s, 1H), 7.73 (m, 2H), 7.55 (t, 1H, J=7.7), 7.43 (m, 1H), 3.76 (s, 3H).

Part E. Preparation of 2-(t-butylaminosulfonyl)phenylboronic Acid.

To a solution of 206.5 g (0.968 mol) of benzene-(N-t-butyl)sulfonamide in 2500 mL of THF under N₂ was added 790 mL (1.98 mol) of 2.5M n-butyllithium in hexane over 35 minutes, keeping the temperature between 0-5° C. The reaction mixture was allowed to warm to 10° C., at which time a thick precipitate formed. Triisopropylborate (305 mL, 1.32 mol) was added keeping the temperature below 35° C. After 1 hour, the reaction mixture was cooled, 1N HCl (1570 mL) was added, and the mixture was stirred overnight. The mixture was extracted with 400 mL of ether three times, and the combined organic extracts were extracted with 500 mL of 1N NaOH three times. The aqueous extracts were acidified to pH 1 with 6N HCl, and then extracted with 500 mL ether three times. The combined ether extracts were dried over MgSO₄, and the solvents evaporated in vacuo until the volume was 700 mL. Hexane (150 mL) was added and overnight, a white precipitate formed. The solid was collected and washed with 10% ether/hexane (250 mL), then dried in vacuo to give 216.3 g (87%) of the desired compound as white crystals. m.p. 118-119° C.; ¹ H NMR (CDCl₃): δ 8.00 (d, 1H); 7.82 (d, 1H); 7.53 (m, 2H); 6.29 (br s, 2H); 5.13 (s, 1H); 1.18 (s, 9H).

Part F. Preparation of 4-amino-21-t-butylaminosulfonyl-[1,1']biphenyl.

A mixture of 3.44 g (20 mmol) of 4-bromoaniline and 5.14 g (20 mmol) of 2-(t-butylaminosulfonyl)phenylboronic acid, 1.16 g of tetrakis(triphenylphosphine) palladium(O) (1 mmol), 0.32 g of tetrabutylammonium bromide (1 mmol) and 20 mL of 2M aqueous sodium carbonate were refluxed with 180 mL of benzene under N₂ for 5.5 hours. After cooling, the mixture was diluted with methylene chloride and water. The two phases were separated and the organic phase was washed with water, dried with MgSO₄ and concentrated in vacuo. The resulting thick oil was chromatographed on silica with 30% EtOAc/hexane to afford 2.52 g (41%) of the aniline. ¹ H NMR (CDCl₃): δ 8.14 (d, 1H); 7.53 (t, 1H); 7.43 (t, 1H); 7.33 (d, 2H); 7.27 (d, 1H); 6.76 (d, 2H); 3.7 (br s, 1H); 0.99 (s, 9H).

Part G. Preparation of N-(2'-t-butylaminosulfonyl-[1,1']biphen-4-yl) -2-(3'-cyanophenyl)nicotinamide.

Methyl 2-(3'-cyanophenyl)nicotinate (300 mg, 1.3 mmol) was combined with of 4-amino-2'-t-butylaminosulfonyl-[1,1']biphenyl (383 mg, 1.3 mmol) in 12 mL dry CH₂ Cl₂. A solution of trimethylaluminum (3.8 mL, 2.0 M in heptane) was added, and an exothermic reaction immediately occurred and the mixture darkened. The resulting solution was stirred at room temperature under argon for 3 days and then quenched carefully with a few drops of 1 M HCl. An emulsion was obtained on dilution with EtOAc and water. The layers were separated, and the organic was extracted again with water and brine, dried over Na₂ SO₄, filtered, and evaporated. A small amount of additional material was obtained from the aqueous extract by adjusting the pH to 8 with sat. NaHCO₃ and extracting with EtOAc. This material was dried over Na₂ SO₄, filtered, evaporated, and combined with the previous extract for chromatography on silica gel (50-60% EtOAc/hexanes) to yield the desired product (190 mg, 30%). ¹ H NMR (CDCl₃): δ 8.86 (dd, 1H, J=4.7, J'=1.9), 8.14 (m, 3H), 8.00 (d, 1H, J=7.7), 7.73 (d, 1H, J=8.1), 7.50 (m, 9H), 7.29 (dd, 1H, J=7.4, J'=1.1), 3.60 (s, 1H), 1.02 (s, 9H).

Part H. Preparation of N-(2'-aminosulfonyl-[1,1']biphen-4-yl)-2-(3'-amidinophenyl)nicotinamide, trifluoroacetic acid Salt.

N-(2'-t-butylaminosulfonyl-[1,1']biphen-4-yl)-2-(3'-cyanophenyl)nicotinamide (190 mg, 0.37 mmol) was dissolved in dry MeOH (10 mL) and cooled to 0° C. HCl(g) was generated by the addition of concentrated H₂ SO₄ (60 mL) to NaCl (240 g) over 40 minutes and was bubbled into the reaction mixture. The gas was permitted to continue bubbling through the reaction for 3 hours after the H₂ SO₄ addition was complete. At this point, the HCl generator and ice bath were removed, and the reaction stirred under argon for 19 hours. This solution was then evaporated, placed under high vacuum, and redissolved in dry MeOH (10 mL). Ammonium carbonate (200 mg) was added, stirred for 24 hours under argon, and evaporated. The product was purified by preparative HPLC on a C-18 reverse phase column (10-70% MeCN/H₂ O/0.05% TFA), yielding a white powder (140 mg, 54%). ¹ H NMR (DMSO-d₆): δ 10.65 (s, 1H), 9.38 (s, 2H), 8.92 (s, 2H), 8.81 (dd, 1H, J=4.4, J'=1.4), 8.10 (m, 2H), 7.97 (m, 2H), 7.76 (m, 1H), 7.67 (t, 1H, J=8.0), 7.57 (m, 5H), 7.29 (m, 5H). HRMS calc. for C₂₅ H₂₂ N₅ O₃ S: m/z 472.1443; found, 472.1457.

Examples 2, 3 and 4 N-[5-(2-aminosulfonyl)phenylpyrid-2-yl]-2-(3'-amidinophenyl)nicotinamide, trifluoroacetic acid salt (Example 2), N-[5-(2-t-butylaminosulfonyl)phenylpyrid-2-yl]-2-(3'-amidinophenyl)nicotinamide, trifluoroacetic acid salt (Example 3), and N-[5-(2-aminosulfonyl)phenylpyrid-2-yl]-2-(3'-carboxamidophenyl)nicotinanside, trifluoroacetic acid salt Example 4

Part A. Preparation of 2-(3'-cyanophenyl)nicotinic acid.

Methyl 2-(3'-cyanophenyl)nicotinate (1.21 g, 5.1 mmol) was partially dissolved in MeOH (40 mL), and lithium hydroxide monohydrate (234 mg dissolved in 6 mL H₂ O, 5.6 mmol) was added. After 20 hours, the resulting solution was diluted with water and extracted with CHCl₃. The aqueous was acidified to pH 4 with 1 M HCl and extracted several times with CHCl₃. Solid sodium chloride was added to the aqueous solution and the solution was extracted with 5-10% MeOH/CHCl₃. The organic extracts were combined, dried over Na₂ SO₄, filtered, and evaporated to yield a white solid (1.06 g, 93%).

¹ H NMR (CDCl₃): δ 8.85 (dd, 1H, J=5.1, J'=1.5), 8.35 (dd, 1H, J=7.6, J'=1.4), 7.84 (s, 1H), 7.75 (m, 2H), 7.55 (t, 1H, J=7.7), 7.47 (m, 1H).

Part B. Preparation of 2-amino-5-(2-t-butylaminosulfonyl)phenylpyridine.

A mixture of 1.55 g (9.0 mmol) of 2-amino-5-bromopyridine and 2.3 g (9.0 mmol) of 2-(t-butylaminosulfonyl)phenylboronic acid, 0.52 g of tetrakis(triphenylphosphine) palladium(O) (0.45 mmol), 0.15 g of tetrabutylammonium bromide (0.45 mmol) and 9 mL of 2M aqueous sodium carbonate were refluxed with 80 mL of benzene under Ar for 5 hours. After cooling, the mixture was diluted with 25 mL of methylene chloride and 25 mL of water. The two phases were separated and the organic phase was washed with water, dried with MgSO₄ and concentrated in vacuo. The resulting thick oil was chromatographed on silica with 50% EtOAc/hexane to afford 1.34 g (49%) of the aniline.

¹ H NMR (CDCl₃): δ 8.18 (d, 1H); 8.07 (m, 1H); 7.70 (dd, 1H); 7.58 (dt, 1H); 7.48 (dt, 1H); 7.28 (d, 1H); 6.56 (d, 1H); 4.62 (br s, 2H); 3.88 (br s, 1H); 1.06 (s, 9H).

Part C. Preparation of N-[5-(2-t-butylaminosulfonyl)phenylpyrid-2-yl]-2-(3'-cyanophenyl)nicotinamide.

2-(3'-cyanophenyl)nicotinic acid (300 mg, 1.3 mmol) was suspended in 5 mL dry CH₂ Cl₂, and oxalyl chloride (175 μl, 2.0 mmol) was added, followed by 2 drops of dry DES. The reaction stirred at room temperature under argon for 2 hours and then evaporated. This solid was redissolved in 8 mL dry CH₂ Cl₂, and dimethylaminopyridine (490 mg, 4.0 mmol) was added, followed by 2-amino-5-(2-t-butylaminosulfonyl)phenylpyridine (410 mg, 1.3 mmol). The reaction was stirred 3 days at room temperature, diluted with CH₂ Cl₂, extracted with saturated NaHCO₃, dried over Na₂ SO₄, filtered, and evaporated. The resulting material was chromatographed on silica gel (50-75% EtOAc/hexanes) to yield the desired product (423 mg, 62%).

¹ H NMR (CDCl₃): δ 8.83 (dd, 1H, J=4.8, J'=1.5), 8.40 (bs, 1H), 8.29 (bd, 1H, J=8.4), 8.17 (dd, 1H), J=8.0, J'=1.1), 8.09 (m, 3H), 7.97 (d, 1H, J=7.7), 7.79 (d, 1H, J=8.4), 7.69 (d, 1H, J=7.7), 7.54 (m, 4H), 7.25 (m, 1H), 4.19 (bs, 1H), 1.08 (s, 9H).

Part D. Preparation of N-[5-(2-aminosulfonyl)phenylpyrid-2-yl]-2-(3'-amidinophenyl)nicotinamide, trifluoroacetic acid salt (Example 2), N-[5-(2-t-butylaminosulfonyl)phenylpyrid-2-yl]-2-(3'-amidinophenyl)nicotinamide, trifluoroacetic acid salt (Example 3), and N-[5-(2-aminosulfonyl)phenylpyrid-2-yl]-2-(3'-carboxamidophenyl)nicotinamide, trifluoroacetic acid salt (Example 4).

N-[5-(2-t-butylaminosulfonyl)phenylpyrid-2-yl]-2-(3'-cyanophenyl)nicotinamide (410 mg, 1.03) was dissolved in a mixture of dry MeOH (5 mL) and dry CHCl₃ (15 mL) and cooled to 0° C. HCl(g) was generated by the addition of concentrated H₂ SO₄ (45 mL) to NaCl (220 g) over 55 min and was bubbled into the reaction mixture. The HCl generator and ice bath were removed, and the reaction was stirred under argon for 16 hours and evaporated. The resulting solid was redissolved in dry MeOH (15 mL), and ammonium carbonate (385 mg) was added. The reaction was stirred 19 hours at room temperature under argon and evaporated. The resulting solid was purified by preparative HPLC on a C-18 reverse phase column (5-70% MeCN/H₂ O/0.05% TFA) to yield N-[5-(2-aminosulfonyl)phenylpyrid-2-yl]-2-(3'-amidinophenyl)nicotinamide, trifluoroacetic acid salt (Example 2), (250 mg, 45%). ¹ H NMR (DMSO-d₆): δ 11.27 (s, 1H), 9.43 (s, 2H), 8.98 (s, 2H), 8.83 (dd, 1H, J=4.8, J'=1.9), 8.32 (s, 1H), 8.13 (m, 2H), 8.05 (m, 2H), 7.96 (d, 1H, J=7.3), 7.81 (d, 2H, J=8.4), 7.65 (m, 4H), 7.47 (s, 2H), 7.37 (m, 1H). HRMS calc. for C₂₄ H₂₁ N₆ O₃ S: m/z 473.1396; found, 473.1397. A second product, N-[5-(2-t-butylaminosulfonyl)-phenylpyrid-2-yl]-2-(3'-amidinophenyl)nicotinamide, trifluoroacetic acid salt (Example 3), was also obtained (58 mg, 10%). ¹ H NMR (DMSO-d₆): δ 9.7 (s, 1H), 9.41 (s, 2H), 8.95 (s, 2H), 8.82 (m, 1H), 8.28 (s, 1H), 8.09 (m, 4H), 7.95 (d, 1H, J=7.7), 7.79 (m, 2H), 7.63 (m, 4H), 7.34 (d, 1H, J=7.7), 7.18 (s, 1H), 1.04 (s, 9H). HRMS calc. for C₂₈ H₂₉ N₆ O₃ S: 529.2022; found, 529.2050. A third product, N-[5-(2-aminosulfonyl)phenylpyrid-2-yl]-2-(3'-carboxamidophenyl)nicotinamide, trifluoroacetic acid salt (Example 4) was isolated and chromatographed on silica gel (10-20% MeOH/CHCl₃) to yield a white solid (77 mg, 20%). ¹ H NMR (DMSO-d₆): δ 11.13 (s, 1H), 8.75 (dd, 1H, J=4.8, J'=1.9), 8.26 (m, 2H), 8.02 (m, 4H), 7.84 (d, 1H, J=7.7), 7.74 (m, 2H), 7.59 (m, 2H), 7.47 (m, 2H), 7.36 (m, 4H).

                  TABLE 1                                                          ______________________________________                                           #STR27##                                                                        -                                 MS                                          Ex D R.sub.2 A' (M + H).sup.+                                                ______________________________________                                         1      C(═NH)NH.sub.2                                                                         SO.sub.2 NH.sub.2                                                                          CH  472.1                                         2 C(═NH)NH.sub.2 SO.sub.2 NH.sub.2 N 473.1                                 3 C(═NH)NH.sub.2 SO.sub.2 NHtBu N 529.2                                    4 C(O)NH.sub.2 SO.sub.2 NH.sub.2 N 474.1                                     ______________________________________                                    

The following table contains representative examples of the present invention. Each entry in the table is intended to be paired with each formulae at the start of the table. For example, example 1 in Table 2 is intended to be paired with each of formulae a₁ -ss₄.

                                      TABLE 2                                      __________________________________________________________________________      ##STR28##                                                                     __________________________________________________________________________                                                 #STR29##                                                                       #STR30##                                                                      ##STR31##                           __________________________________________________________________________     a.sub.1                                                                           R = F, D = NH.sub.2                                                                              b.sub.1                                                                           R = F, D = NH.sub.2                                                                              c.sub.1                                                                           R = F, D = NH.sub.2                 a.sub.2 R = H, D = NH.sub.2 b.sub.2 R = H, D = NH.sub.2 c.sub.2 R = H,                                                    D = NH.sub.2                        a.sub.3 R = F, D = CH.sub.2 NH.sub.2 b.sub.3 R = F, D = CH.sub.2                                                          NH.sub.2 c.sub.3 R = F, D =                                                    CH.sub.2 NH.sub.2                   a.sub.4 R = H, D = CH.sub.2 NH.sub.2 b.sub.4 R = H, D = CH.sub.2                                                          NH.sub.2 c.sub.4 R = H, D =                                                    CH.sub.2 NH.sub.2                   a.sub.5 R = F, D = C(═NH)NH.sub.2 b.sub.5 R = F, D = C(═NH)NH.su                                                  b.2 c.sub.5 R = F, D =                                                         C(═NH)NH.sub.2                  a.sub.6 R = H, D = C(═NH)NH.sub.2 b.sub.6 R = H, D = C(═NH)NH.su                                                  b.2 c.sub.6 R = H, D =                                                         C(═NH)NH.sub.2                  a.sub.7 R = F, D = C(O)NH.sub.2 b.sub.7 R = F, D = C(O)NH.sub.2 c.sub.7                                                   R = F, D = C(O)NH.sub.2                                                         a.sub.8 R = H, D = C(O)NH.su                                                  b.2 b.sub.8 R = H, D =                                                         C(O)NH.sub.2 c.sub.8 R = H,                                                    D = C(O)NH.sub.2                  __________________________________________________________________________                                                 #STR32##                                                                       #STR33##                                                                      ##STR34##                           __________________________________________________________________________     d.sub.1                                                                           R = F, D = NH.sub.2                                                                              e.sub.1                                                                           R = F, D = NH.sub.2                                                                              f.sub.1                                                                           R = F, D = NH.sub.2                 d.sub.2 R = H, D = NH.sub.2 e.sub.2 R = H, D = NH.sub.2 f.sub.2 R = H,                                                    D = NH.sub.2                        d.sub.3 R = F, D = CH.sub.2 NH.sub.2 e.sub.3 R = F, D = CH.sub.2                                                          NH.sub.2 f.sub.3 R = F, D =                                                    CH.sub.2 NH.sub.2                   d.sub.4 R = H, D = CH.sub.2 NH.sub.2 e.sub.4 R = H, D = CH.sub.2                                                          NH.sub.2 f.sub.4 R = H, D =                                                    CH.sub.2 NH.sub.2                   d.sub.5 R = F, D = C(═NH)NH.sub.2 e.sub.5 R = F, D = C(═NH)NH.su                                                  b.2 f.sub.5 R = F, D =                                                         C(═NH)NH.sub.2                  d.sub.6 R = H, D = C(═NH)NH.sub.2 e.sub.6 R = H, D = C(═NH)NH.su                                                  b.2 f.sub.6 R = H, D =                                                         C(═NH)NH.sub.2                  d.sub.7 R = F, D = C(O)NH.sub.2 e.sub.7 R = F, D = C(O)NH.sub.2 f.sub.7                                                   R = F, D = C(O)NH.sub.2                                                         d.sub.8 R = H, D = C(O)NH.su                                                  b.2 e.sub.8 R = H, D =                                                         C(O)NH.sub.2 f.sub.8 R = H,                                                    D = C(O)NH.sub.2                  __________________________________________________________________________                                                 #STR35##                                                                       #STR36##                                                                      ##STR37##                           __________________________________________________________________________     g.sub.1                                                                           R = F, D = NH.sub.2                                                                              h.sub.1                                                                           R = F, D = NH.sub.2                                                                              i.sub.1                                                                           R = F, D = NH.sub.2                 g.sub.2 R = H, D = NH.sub.2 h.sub.2 R = H, D = NH.sub.2 i.sub.2 R = H,                                                    D = NH.sub.2                        g.sub.3 R = F, D = CH.sub.2 NH.sub.2 h.sub.3 R = F, D = CH.sub.2                                                          NH.sub.2 i.sub.3 R = F, D =                                                    CH.sub.2 NH.sub.2                   g.sub.4 R = H, D = CH.sub.2 NH.sub.2 h.sub.4 R = H, D = CH.sub.2                                                          NH.sub.2 i.sub.4 R = H, D =                                                    CH.sub.2 NH.sub.2                   g.sub.5 R = F, D = C(═NH)NH.sub.2 h.sub.5 R = F, D = C(═NH)NH.su                                                  b.2 i.sub.5 R = F, D =                                                         C(═NH)NH.sub.2                  g.sub.6 R = H, D = C(═NH)NH.sub.2 h.sub.6 R = H, D = C(═NH)NH.su                                                  b.2 i.sub.6 R = H, D =                                                         C(═NH)NH.sub.2                  g.sub.7 R = F, D = C(O)NH.sub.2 h.sub.7 R = F, D = C(O)NH.sub.2 i.sub.7                                                   R = F, D = C(O)NH.sub.2                                                         g.sub.8 R = H, D = C(O)NH.su                                                  b.2 h.sub.8 R = H, D =                                                         C(O)NH.sub.2 i.sub.8 R = H,                                                    D = C(O)NH.sub.2                  __________________________________________________________________________                                                 #STR38##                                                                       #STR39##                                                                      ##STR40##                           __________________________________________________________________________     j.sub.1                                                                           R = F, D = NH.sub.2                                                                              k.sub.1                                                                           R = F, D = NH.sub.2                                                                              l.sub.1                                                                           R = F, D = NH.sub.2                 j.sub.2 R = H, D = NH.sub.2 k.sub.2 R = H, D = NH.sub.2 l.sub.2 R = H,                                                    D = NH.sub.2                        j.sub.3 R = F, D = CH.sub.2 NH.sub.2 k.sub.3 R = F, D = CH.sub.2                                                          NH.sub.2 l.sub.3 R = F, D =                                                    CH.sub.2 NH.sub.2                   j.sub.4 R = H, D = CH.sub.2 NH.sub.2 k.sub.4 R = H, D = CH.sub.2                                                          NH.sub.2 l.sub.4 R = H, D =                                                    CH.sub.2 NH.sub.2                   j.sub.5 R = F, D = C(═NH)NH.sub.2 k.sub.5 R = F, D = C(═NH)NH.su                                                  b.2 l.sub.5 R = F, D =                                                         C(═NH)NH.sub.2                  j.sub.6 R = H, D = C(═NH)NH.sub.2 k.sub.6 R = H, D = C(═NH)NH.su                                                  b.2 l.sub.6 R = H, D =                                                         C(═NH)NH.sub.2                  j.sub.7 R = F, D = C(O)NH.sub.2 k.sub.7 R = F, D = C(O)NH.sub.2 l.sub.7                                                   R = F, D = C(O)NH.sub.2                                                         j.sub.8 R = H, D = C(O)NH.su                                                  b.2 k.sub.8 R = H, D =                                                         C(O)NH.sub.2 l.sub.8 R = H,                                                    D = C(O)NH.sub.2                  __________________________________________________________________________                                                 #STR41##                                                                       #STR42##                                                                      ##STR43##                           __________________________________________________________________________     m.sub.1                                                                           R = F, D = NH.sub.2                                                                              n.sub.1                                                                           R = F, D = NH.sub.2                                                                              o.sub.1                                                                           R = F, D = NH.sub.2                 m.sub.2 R = H, D = NH.sub.2 n.sub.2 R = H, D = NH.sub.2 o.sub.2 R = H,                                                    D = NH.sub.2                        m.sub.3 R = F, D = CH.sub.2 NH.sub.2 n.sub.3 R = F, D = CH.sub.2                                                          NH.sub.2 o.sub.3 R = F, D =                                                    CH.sub.2 NH.sub.2                   m.sub.4 R = H, D = CH.sub.2 NH.sub.2 n.sub.4 R = H, D = CH.sub.2                                                          NH.sub.2 o.sub.4 R = H, D =                                                    CH.sub.2 NH.sub.2                   m.sub.5 R = F, D = C(═NH)NH.sub.2 n.sub.5 R = F, D = C(═NH)NH.su                                                  b.2 o.sub.5 R = F, D =                                                         C(═NH)NH.sub.2                  m.sub.6 R = H, D = C(═NH)NH.sub.2 n.sub.6 R = H, D = C(═NH)NH.su                                                  b.2 o.sub.6 R = H, D =                                                         C(═NH)NH.sub.2                  m.sub.7 R = F, D = C(O)NH.sub.2 n.sub.7 R = F, D = C(O)NH.sub.2 o.sub.7                                                   R = F, D = C(O)NH.sub.2                                                         m.sub.8 R = H, D = C(O)NH.su                                                  b.2 n.sub.8 R = H, D =                                                         C(O)NH.sub.2 o.sub.8 R = H,                                                    D = C(O)NH.sub.2                  __________________________________________________________________________                                                 #STR44##                                                                       #STR45##                                                                      ##STR46##                           __________________________________________________________________________     p.sub.1                                                                           R = F, D = NH.sub.2                                                                              q.sub.1                                                                           R = F, D = NH.sub.2                                                                              r.sub.1                                                                           R = F, D = NH.sub.2                 p.sub.2 R = Cl, D = NH.sub.2 q.sub.2 R = Cl, D = NH.sub.2 r.sub.2 R =                                                     Cl, D = NH.sub.2                    p.sub.3 R = OMe, D = NH.sub.2 q.sub.3 R = OMe, D = NH.sub.2 r.sub.3 R =                                                   OMe, D = NH.sub.2                   p.sub.4 R = F, D = CH.sub.2 NH.sub.2 q.sub.4 R = F, D = CH.sub.2                                                          NH.sub.2 r.sub.4 R = F, D =                                                    CH.sub.2 NH.sub.2                   p.sub.5 R = Cl, D = CH.sub.2 NH.sub.2 q.sub.5 R = Cl, D = CH.sub.2                                                        NH.sub.2 r.sub.5 R = Cl, D =                                                   CH.sub.2 NH.sub.2                   p.sub.6 R = OMe, D = CH.sub.2 NH.sub.2 q.sub.6 R = OMe, D = CH.sub.2                                                      NH.sub.2 r.sub.6 R = OMe, D                                                    = CH.sub.2 NH.sub.2                 p.sub.7 R = F, D = C(═NH)NH.sub.2 q.sub.7 R = F, D = C(═NH)NH.su                                                  b.2 r.sub.7 R = F, D =                                                         C(═NH)NH.sub.2                  p.sub.8 R = Cl, D = C(═NH)NH.sub.2 q.sub.8 R = Cl, D = C(═NH)NH.                                                  sub.2 r.sub.8 R = Cl, D =                                                      C(═NH)NH.sub.2                  p.sub.9 R = OMe, D = C(═NH)NH.sub.2 q.sub.9 R = OMe, D = C(═NH)N                                                  H.sub.2 r.sub.9 R = OMe, D =                                                   C(═NH)NH.sub.2                  p.sub.10 R = F, D = C(O)NH.sub.2 q.sub.10 R = F, D = C(O)NH.sub.2                                                         r.sub.10 R = F, D = C(O)NH.su                                                  b.2                                 p.sub.11 R = Cl, D = C(O)NH.sub.2 q.sub.11 R = Cl, D = C(O)NH.sub.2                                                       r.sub.11 R = Cl, D =                                                           C(O)NH.sub.2                        p.sub.12 R = OMe, D = C(O)NH.sub.2 q.sub.12 R = OMe, D = C(O)NH.sub.2                                                     r.sub.12 R = OMe, D =                                                          C(O)NH.sub.2                      __________________________________________________________________________                                                 #STR47##                                                                       #STR48##                                                                      ##STR49##                           __________________________________________________________________________     s.sub.1                                                                           R = F, D = NH.sub.2                                                                              t.sub.1                                                                           R = F, D = NH.sub.2                                                                              u.sub.1                                                                           R = F, D = NH.sub.2                 s.sub.2 R = Cl, D = NH.sub.2 t.sub.2 R = Cl, D = NH.sub.2 u.sub.2 R =                                                     Cl, D = NH.sub.2                    s.sub.3 R = OMe, D = NH.sub.2 t.sub.3 R = OMe, D = NH.sub.2 u.sub.3 R =                                                   OMe, D = NH.sub.2                   s.sub.4 R = F, D = CH.sub.2 NH.sub.2 t.sub.4 R = F, D = CH.sub.2                                                          NH.sub.2 u.sub.4 R = F, D =                                                    CH.sub.2 NH.sub.2                   s.sub.5 R = Cl, D = CH.sub.2 NH.sub.2 t.sub.5 R = Cl, D = CH.sub.2                                                        NH.sub.2 u.sub.5 R = Cl, D =                                                   CH.sub.2 NH.sub.2                   s.sub.6 R = OMe, D = CH.sub.2 NH.sub.2 t.sub.6 R = OMe, D = CH.sub.2                                                      NH.sub.2 u.sub.6 R = OMe, D                                                    = CH.sub.2 NH.sub.2                 s.sub.7 R = F, D = C(═NH)NH.sub.2 t.sub.7 R = F, D = C(═NH)NH.su                                                  b.2 u.sub.7 R = F, D =                                                         C(═NH)NH.sub.2                  s.sub.8 R = Cl, D = C(═NH)NH.sub.2 t.sub.8 R = Cl, D = C(═NH)NH.                                                  sub.2 u.sub.8 R = Cl, D =                                                      C(═NH)NH.sub.2                  s.sub.9 R = OMe, D = C(═NH)NH.sub.2 t.sub.9 R = OMe, D = C(═NH)N                                                  H.sub.2 u.sub.9 R = OMe, D =                                                   C(═NH)NH.sub.2                  s.sub.10 R = F, D = C(O)NH.sub.2 t.sub.10 R = F, D = C(O)NH.sub.2                                                         u.sub.10 R = F, D = C(O)NH.su                                                  b.2                                 s.sub.11 R = Cl, D = C(O)NH.sub.2 t.sub.11 R = Cl, D = C(O)NH.sub.2                                                       u.sub.11 R = Cl, D =                                                           C(O)NH.sub.2                        s.sub.12 R = OMe, D = C(O)NH.sub.2 t.sub.12 R = OMe, D = C(O)NH.sub.2                                                     u.sub.12 R = OMe, D =                                                          C(O)NH.sub.2                      __________________________________________________________________________                                                 #STR50##                                                                       #STR51##                                                                      ##STR52##                           __________________________________________________________________________     v.sub.1                                                                           R = F, D = NH.sub.2                                                                              w.sub.1                                                                           R = F, D = NH.sub.2                                                                              x.sub.1                                                                           R = F, D = NH.sub.2                 v.sub.2 R = Cl, D = NH.sub.2 w.sub.2 R = Cl, D = NH.sub.2 x.sub.2 R =                                                     Cl, D = NH.sub.2                    v.sub.3 R = OMe, D = NH.sub.2 w.sub.3 R = OMe, D = NH.sub.2 x.sub.3 R =                                                   OMe, D = NH.sub.2                   v.sub.4 R = F, D = CH.sub.2 NH.sub.2 w.sub.4 R = F, D = CH.sub.2                                                          NH.sub.2 x.sub.4 R = F, D =                                                    CH.sub.2 NH.sub.2                   v.sub.5 R = Cl, D = CH.sub.2 NH.sub.2 w.sub.5 R = Cl, D = CH.sub.2                                                        NH.sub.2 x.sub.5 R = Cl, D =                                                   CH.sub.2 NH.sub.2                   v.sub.6 R = OMe, D = CH.sub.2 NH.sub.2 w.sub.6 R = OMe, D = CH.sub.2                                                      NH.sub.2 x.sub.6 R = OMe, D                                                    = CH.sub.2 NH.sub.2                 v.sub.7 R = F, D = C(═NH)NH.sub.2 w.sub.7 R = F, D = C(═NH)NH.su                                                  b.2 x.sub.7 R = F, D =                                                         C(═NH)NH.sub.2                  v.sub.8 R = Cl, D = C(═NH)NH.sub.2 w.sub.8 R = Cl, D = C(═NH)NH.                                                  sub.2 x.sub.8 R = Cl, D =                                                      C(═NH)NH.sub.2                  v.sub.9 R = OMe, D = C(═NH)NH.sub.2 w.sub.9 R = OMe, D = C(═NH)N                                                  H.sub.2 x.sub.9 R = OMe, D =                                                   C(═NH)NH.sub.2                  v.sub.10 R = F, D = C(O)NH.sub.2 w.sub.10 R = F, D = C(O)NH.sub.2                                                         x.sub.10 R = F, D = C(O)NH.su                                                  b.2                                 v.sub.11 R = Cl, D = C(O)NH.sub.2 w.sub.11 R = Cl, D = C(O)NH.sub.2                                                       x.sub.11 R = Cl, D =                                                           C(O)NH.sub.2                        v.sub.12 R = OMe, D = C(O)NH.sub.2 w.sub.12 R = OMe, D = C(O)NH.sub.2                                                     x.sub.12 R = OMe, D =                                                          C(O)NH.sub.2                      __________________________________________________________________________                                                 #STR53##                                                                       #STR54##                                                                      ##STR55##                           __________________________________________________________________________     y.sub.1                                                                           R = F, D = NH.sub.2                                                                              z.sub.1                                                                           R = F, D = NH.sub.2                                                                              aa.sub.1                                                                          R = F, D = NH.sub.2                 y.sub.2 R = Cl, D = NH.sub.2 z.sub.2 R = Cl, D = NH.sub.2 aa.sub.2 R =                                                    Cl, D = NH.sub.2                    y.sub.3 R = OMe, D = NH.sub.2 z.sub.3 R = OMe, D = NH.sub.2 aa.sub.3 R                                                    = OMe, D = NH.sub.2                 y.sub.4 R = F, D = CH.sub.2 NH.sub.2 z.sub.4 R = F, D = CH.sub.2                                                          NH.sub.2 aa.sub.4 R = F, D =                                                   CH.sub.2 NH.sub.2                   y.sub.5 R = Cl, D = CH.sub.2 NH.sub.2 z.sub.5 R = Cl, D = CH.sub.2                                                        NH.sub.2 aa.sub.5 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 y.sub.6 R = OMe, D = CH.sub.2 NH.sub.2 z.sub.6 R = OMe, D = CH.sub.2                                                      NH.sub.2 aa.sub.6 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 y.sub.7 R = F, D = C(═NH)NH.sub.2 z.sub.7 R = F, D = C(═NH)NH.su                                                  b.2 aa.sub.7 R = F, D =                                                        C(═NH)NH.sub.2                  y.sub.8 R = Cl, D = C(═NH)NH.sub.2 z.sub.8 R = Cl, D = C(═NH)NH.                                                  sub.2 aa.sub.8 R = Cl, D =                                                     C(═NH)NH.sub.2                  y.sub.9 R = OMe, D = C(═NH)NH.sub.2 z.sub.9 R = OMe, D = C(═NH)N                                                  H.sub.2 aa.sub.9 R = OMe, D                                                    = C(═NH)NH.sub.2                                                            y.sub.10 R = F, D =                                                           C(O)NH.sub.2 z.sub.10 R = F,                                                   D = C(O)NH.sub.2 aa.sub.10 R                                                   = F, D = C(O)NH.sub.2                                                           y.sub.11 R = Cl, D =                                                          C(O)NH.sub.2 z.sub.11 R =                                                      Cl, D = C(O)NH.sub.2                                                           aa.sub.11 R = Cl, D =                                                          C(O)NH.sub.2                        y.sub.12 R = OMe, D = C(O)NH.sub.2 z.sub.12 R = OMe, D = C(O)NH.sub.2                                                     aa.sub.12 R = OMe, D =                                                         C(O)NH.sub.2                      __________________________________________________________________________                                                 #STR56##                                                                       #STR57##                                                                      ##STR58##                           __________________________________________________________________________     bb.sub.1                                                                          R = F, D = NH.sub.2                                                                              cc.sub.1                                                                          R = F, D = NH.sub.2                                                                              dd.sub.1                                                                          R = F, D = NH.sub.2                 bb.sub.2 R = Cl, D = NH.sub.2 cc.sub.2 R = Cl, D = NH.sub.2 dd.sub.2 R                                                    = Cl, D = NH.sub.2                  bb.sub.3 R = OMe, D = NH.sub.2 cc.sub.3 R = OMe, D = NH.sub.2 dd.sub.3                                                    R = OMe, D = NH.sub.2                                                           bb.sub.4 R = F, D =                                                           CH.sub.2 NH.sub.2 cc.sub.4 R                                                   = F, D = CH.sub.2 NH.sub.2                                                     dd.sub.4 R = F, D = CH.sub.2                                                   NH.sub.2                            bb.sub.5 R = Cl, D = CH.sub.2 NH.sub.2 cc.sub.5 R = Cl, D = CH.sub.2                                                      NH.sub.2 dd.sub.5 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 bb.sub.6 R = OMe, D = CH.sub.2 NH.sub.2 cc.sub.6 R = OMe, D = CH.sub.2                                                    NH.sub.2 dd.sub.6 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 bb.sub.7 R = F, D = C(═NH)NH.sub.2 cc.sub.7 R = F, D = C(═NH)NH.                                                  sub.2 dd.sub.7 R = F, D =                                                      C(═NH)NH.sub.2                  bb.sub.8 R = Cl, D = C(═NH)NH.sub.2 cc.sub.8 R = Cl, D = C(═NH)N                                                  H.sub.2 dd.sub.8 R = Cl, D =                                                   C(═NH)NH.sub.2                  bb.sub.9 R = OMe, D = C(═NH)NH.sub.2 cc.sub.9 R = OMe, D = C(═NH                                                  )NH.sub.2 dd.sub.9 R = OMe,                                                    D = C(═NH)NH.sub.2                                                          bb.sub.10 R = F, D =                                                          C(O)NH.sub.2 cc.sub.10 R =                                                     F, D = C(O)NH.sub.2 dd.sub.10                                                   R = F, D = C(O)NH.sub.2                                                        bb.sub.11 R = Cl, D =                                                         C(O)NH.sub.2 cc.sub.11 R =                                                     Cl, D = C(O)NH.sub.2                                                           dd.sub.11 R = Cl, D =                                                          C(O)NH.sub.2                        bb.sub.12 R = OMe, D = C(O)NH.sub.2 cc.sub.12 R = OMe, D = C(O)NH.sub.2                                                   dd.sub.12 R = OMe, D =                                                         C(O)NH.sub.2                      __________________________________________________________________________                                                 #STR59##                                                                       #STR60##                                                                      ##STR61##                           __________________________________________________________________________     ee.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     ff.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     gg.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2        ee.sub.2 R = Cl, D = CH.sub.2 NH.sub.2 ff.sub.2 R = Cl, D = CH.sub.2                                                      NH.sub.2 gg.sub.2 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 ee.sub.3 R = OMe, D = CH.sub.2 NH.sub.2 ff.sub.3 R = OMe, D = CH.sub.2                                                    NH.sub.2 gg.sub.3 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 ee.sub.4 R = CH.sub.2 NH.sub.2, ff.sub.4 R = CH.sub.2 NH.sub.2,                                                           gg.sub.4 R = CH.sub.2                                                          NH.sub.2,                            D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2         __________________________________________________________________________                                                 #STR62##                                                                       #STR63##                                                                      ##STR64##                           __________________________________________________________________________     hh.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     ii.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     jj.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2        hh.sub.2 R = Cl, D = CH.sub.2 NH.sub.2 ii.sub.2 R = Cl, D = CH.sub.2                                                      NH.sub.2 jj.sub.2 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 hh.sub.3 R = OMe, D = CH.sub.2 NH.sub.2 ii.sub.3 R = OMe, D = CH.sub.2                                                    NH.sub.2 jj.sub.3 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 hh.sub.4 R = CH.sub.2 NH.sub.2, ii.sub.4 R = CH.sub.2 NH.sub.2,                                                           jj.sub.4 R = CH.sub.2                                                          NH.sub.2,                            D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2         __________________________________________________________________________                                                 #STR65##                                                                       #STR66##                                                                      ##STR67##                           __________________________________________________________________________     kk.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     ll.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     mm.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2        kk.sub.2 R = Cl, D = CH.sub.2 NH.sub.2 ll.sub.2 R = Cl, D = CH.sub.2                                                      NH.sub.2 mm.sub.2 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 kk.sub.3 R = OMe, D = CH.sub.2 NH.sub.2 ll.sub.3 R = OMe, D = CH.sub.2                                                    NH.sub.2 mm.sub.3 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 kk.sub.4 R = CH.sub.2 NH.sub.2, ll.sub.4 R = CH.sub.2 NH.sub.2,                                                           mm.sub.4 R = CH.sub.2                                                          NH.sub.2,                            D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2         __________________________________________________________________________                                                 #STR68##                                                                       #STR69##                                                                      ##STR70##                           __________________________________________________________________________     nn.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     oo.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     pp.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2        nn.sub.2 R = Cl, D = CH.sub.2 NH.sub.2 oo.sub.2 R = Cl, D = CH.sub.2                                                      NH.sub.2 pp.sub.2 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 nn.sub.3 R = OMe, D = CH.sub.2 NH.sub.2 oo.sub.3 R = OMe, D = CH.sub.2                                                    NH.sub.2 pp.sub.3 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 nn.sub.4 R = CH.sub.2 NH.sub.2, oo.sub.4 R = CH.sub.2 NH.sub.2,                                                           pp.sub.4 R = CH.sub.2                                                          NH.sub.2,                            D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2         __________________________________________________________________________                                                 #STR71##                                                                       #STR72##                                                                      ##STR73##                           __________________________________________________________________________     qq.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     rr.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     ss.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2        qq.sub.2 R = Cl, D = CH.sub.2 NH.sub.2 rr.sub.2 R = Cl, D = CH.sub.2                                                      NH.sub.2 ss.sub.2 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 qq.sub.3 R = OMe, D = CH.sub.2 NH.sub.2 rr.sub.3 R = OMe, D = CH.sub.2                                                    NH.sub.2 ss.sub.3 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 qq.sub.4 R = CH.sub.2 NH.sub.2, rr.sub.4 R = CH.sub.2 NH.sub.2,                                                           ss.sub.4 R = CH.sub.2                                                          NH.sub.2,                            D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2         __________________________________________________________________________

    ______________________________________                                         Ex # R.sup.1b  A          B                                                    ______________________________________                                         1    H         phenyl     2-(aminosulfonyl)phenyl                                2 H phenyl 2-(methylaminosulfonyl)phenyl                                       3 H phenyl 1-pyrrolidinocarbonyl                                               4 H phenyl 2-(methylsulfonyl)phenyl                                            5 H phenyl 4-morpholino                                                        6 H phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                7 H phenyl 4-morpholinocarbonyl                                                8 H 2-pyridyl 2-(aminosulfonyl)phenyl                                          9 H 2-pyridyl 2-(methylaminosulfonyl)phenyl                                    10 H 2-pyridyl 1-pyrrolidinocarbonyl                                           11 H 2-pyridyl 2-(methylsulfonyl)phenyl                                        12 H 2-pyridyl 4-morpholino                                                    13 H 2-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                            14 H 2-pyridyl 4-morpholinocarbonyl                                            15 H 3-pyridyl 2-(aminosulfonyl)phenyl                                         16 H 3-pyridyl 2-(methylaminosulfonyl)phenyl                                   17 H 3-pyridyl 1-pyrrolidinocarbonyl                                           18 H 3-pyridyl 2-(methylsulfonyl)phenyl                                        19 H 3-pyridyl 4-morpholino                                                    20 H 3-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                            21 H 3-pyridyl 4-morpholinocarbonyl                                            22 H 2-pyrimidyl 2-(aminosulfonyl)phenyl                                       23 H 2-pyrimidyl 2-(methylaminosulfonyl)phenyl                                 24 H 2-pyrimidyl 1-pyrrolidinocarbonyl                                         25 H 2-pyrimidyl 2-(methylsulfonyl)phenyl                                      26 H 2-pyrimidyl 4-morpholino                                                  27 H 2-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                          28 H 2-pyrimidyl 4-morpholinocarbonyl                                          29 H 5-pyrimidyl 2-(aminosulfonyl)phenyl                                       30 H 5-pyrimidyl 2-(methylaminosulfonyl)phenyl                                 31 H 5-pyrimidyl 1-pyrrolidinocarbonyl                                         32 H 5-pyrimidyl 2-(methylsulfonyl)phenyl                                      33 H 5-pyrimidyl 4-morpholino                                                  34 H 5-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                          35 H 5-pyrimidyl 4-morpholinocarbonyl                                          36 H 2-Cl-phenyl 2-(aminosulfonyl)phenyl                                       37 H 2-Cl-phenyl 2-(methylaminosulfonyl)phenyl                                 38 H 2-Cl-phenyl 1-pyrrolidinocarbonyl                                         39 H 2-Cl-phenyl 2-(methylsulfonyl)phenyl                                      40 H 2-Cl-phenyl 4-morpholino                                                  41 H 2-Cl-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                          42 H 2-Cl-phenyl 4-morpholinocarbonyl                                          43 H 2-F-phenyl 2-(aminosulfonyl)phenyl                                        44 H 2-F-phenyl 2-(methylaminosulfonyl)phenyl                                  45 H 2-F-phenyl 1-pyrrolidinocarbonyl                                          46 H 2-F-phenyl 2-(methylsulfonyl)phenyl                                       47 H 2-F-phenyl 4-morpholino                                                   48 H 2-F-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                           49 H 2-F-phenyl 4-morpholinocarbonyl                                           50 H 2,5-diF-phenyl 2-(aminosulfonyl)phenyl                                    51 H 2,5-diF-phenyl 2-(methylaminosulfonyl)phenyl                              52 H 2,5-diF-phenyl 1-pyrrolidinocarbonyl                                      53 H 2,5-diF-phenyl 2-(methylsulfonyl)phenyl                                   54 H 2,5-diF-phenyl 4-morpholino                                               55 H 2,5-diF-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                       56 H 2,5-diF-phenyl 4-morpholinocarbonyl                                       57 H phenyl 2-(N-pyrrolidinyl-methyl)phenyl                                    58 H phenyl 2-(N-piperidinyl-methyl)phenyl                                     59 H phenyl 2-(N-morpholino-methyl)phenyl                                      60 H phenyl 2-(N,N'-methylmorpholinium-                                           methyl)phenyl                                                               61 H phenyl 2-(N-pyridinium-methyl)phenyl                                      62 H phenyl 2-(N-4-(N,N'-dimethylamino)-                                          pyridinium-methyl)phenyl                                                    63 H phenyl 2-(N-azatanyl-methyl)phenyl                                        64 H phenyl 2-(N-azetidinyl-methyl)phenyl                                      65 H phenyl 2-(N-piperazinyl-methyl)phenyl                                     66 H phenyl 2-(N,N'-BOC-piperazinyl-                                              methyl)phenyl                                                               67 H phenyl 2-(N-imidazolyl-methyl)phenyl                                      68 H phenyl 2-(N-methoxy-N-methylamino-                                           methyl)phenyl                                                               69 H phenyl 2-(N-pyridonyl-methyl)phenyl                                       70 H phenyl 2-(N-(N',N'-dimethylhydrazinyl-                                       methyl)phenyl                                                               71 H phenyl 2-(amidinyl)phenyl                                                 72 H phenyl 2-(N-guanidinyl)phenyl                                             73 H phenyl 2-(imidazolyl)phenyl                                               74 H phenyl 2-(imidazolidinyl)phenyl                                           75 H phenyl 2-(2-imidazolidinyl-                                                  sulfonyl)phenyl                                                             76 H phenyl 2-(2-pyrrolidinyl)phenyl                                           77 H phenyl 2-(2-piperidinyl)phenyl                                            78 H phenyl 2-(amidinyl-methyl)phenyl                                          79 H phenyl 2-(2-imidazolidinyl-                                                  methyl)phenyl                                                               80 H phenyl 2-(N-(2-aminoimidazolyl)-                                             methyl)phenyl                                                               81 H phenyl 2-dimethylaminoimidazol-1-yl                                       82 H phenyl 2-(3-aminophenyl)                                                  83 H phenyl 2-(3-pyrrolidinylcarbonyl)                                         84 H phenyl 2-glycinoyl                                                        85 H phenyl 2-(imidazol-1-ylacetyl)                                            86 H 2-pyridyl 2-(N-pyrrolidinyl-methyl)phenyl                                 87 H 2-pyridyl 2-(N-piperidinyl-methyl)phenyl                                  88 H 2-pyridyl 2-(N-morpholino-methyl)phenyl                                   89 H 2-pyridyl 2-(N,N'-methylmorpholinium-                                        methyl)phenyl                                                               90 H 2-pyridyl 2-(N-pyridinium-methyl)phenyl                                   91 H 2-pyridyl 2-(N-4-(N,N'-dimethylamino)-                                       pyridinium-methyl)phenyl                                                    92 H 2-pyridyl 2-(N-azatanyl-methyl)phenyl                                     93 H 2-pyridyl 2-(N-azetidinyl-methyl)phenyl                                   94 H 2-pyridyl 2-(N-piperazinyl-methyl)phenyl                                  95 H 2-pyridyl 2-(N,N'-BOC-piperazinyl-                                           methyl)phenyl                                                               96 H 2-pyridyl 2-(N-imidazolyl-methyl)phenyl                                   97 H 2-pyridyl 2-(N-methoxy-N-methylamino-                                        methyl)phenyl                                                               98 H 2-pyridyl 2-(N-pyridonyl-methyl)phenyl                                    99 H 2-pyridyl 2-(N-(N',N'-dimethylhydrazinyl-                                    methyl)phenyl                                                               100 H 2-pyridyl 2-(amidinyl)phenyl                                             101 H 2-pyridyl 2-(N-guanidinyl)phenyl                                         102 H 2-pyridyl 2-(imidazolyl)phenyl                                           103 H 2-pyridyl 2-(imidazolidinyl)phenyl                                       104 H 2-pyridyl 2-(2-imidazolidinyl-                                              sulfonyl)phenyl                                                             105 H 2-pyridyl 2-(2-pyrrolidinyl)phenyl                                       106 H 2-pyridyl 2-(2-piperidinyl)phenyl                                        107 H 2-pyridyl 2-(amidinyl-methyl)phenyl                                      108 H 2-pyridyl 2-(2-imidazolidinyl-                                              methyl)phenyl                                                               109 H 2-pyridyl 2-(N-(2-aminoimidazolyl)-                                         methyl)phenyl                                                               110 H 2-pyridyl 2-dimethylaminoimidazol-1-yl                                   111 H 2-pyridyl 2-(3-aminophenyl)                                              112 H 2-pyridyl 2-(3-pyrrolidinylcarbonyl)                                     113 H 2-pyridyl 2-glycinoyl                                                    114 H 2-pyridyl 2-(imidazol-1-ylacetyl)                                        115 H 3-pyridyl 2-(N-pyrrolidinyl-methyl)phenyl                                116 H 3-pyridyl 2-(N-piperidinyl-methyl)phenyl                                 117 H 3-pyridyl 2-(N-morpholino-methyl)phenyl                                  118 H 3-pyridyl 2-(N,N'-methylmorpholinium-                                       methyl)phenyl                                                               119 H 3-pyridyl 2-(N-pyridiniuin-methyl)phenyl                                 120 H 3-pyridyl 2-(N-4-(N,N'-dimethylamino)-                                      pyridinium-methyl)phenyl                                                    121 H 3-pyridyl 2-(N-azatanyl-methyl)phenyl                                    122 H 3-pyridyl 2-(N-azetidinyl-methyl)phenyl                                  123 H 3-pyridyl 2-(N-piperazinyl-methyl)phenyl                                 124 H 3-pyridyl 2-(N,N'-BOC-piperazinyl-                                          methyl)phenyl                                                               125 H 3-pyridyl 2-(N-imidazolyl-methyl)phenyl                                  126 H 3-pyridyl 2-(N-methoxy-N-methylamino-                                       methyl)phenyl                                                               127 H 3-pyridyl 2-(N-pyridonyl-methyl)phenyl                                   128 H 3-pyridyl 2-(N-(N',N'-dimethylhydrazinyl-                                   methyl)phenyl                                                               129 H 3-pyridyl 2-(amidinyl)phenyl                                             130 H 3-pyridyl 2-(N-guanidinyl)phenyl                                         131 H 3-pyridyl 2-(imidazolyl)phenyl                                           132 H 3-pyridyl 2-(imidazolidinyl)phenyl                                       133 H 3-pyridyl 2-(2-imidazolidinyl-                                              sulfonyl)phenyl                                                             134 H 3-pyridyl 2-(2-pyrrolidinyl)phenyl                                       135 H 3-pyridyl 2-(2-piperidinyl)phenyl                                        136 H 3-pyridyl 2-(amidinyl-methyl)phenyl                                      137 H 3-pyridyl 2-(2-imidazolidinyl-                                              methyl)phenyl                                                               138 H 3-pyridyl 2-(N-(2-aminoimidazolyl)-                                         methyl)phenyl                                                               139 H 3-pyridyl 2-dimethylaminoimidazol-1-yl                                   140 H 3-pyridyl 2-(3-aminophenyl)                                              141 H 3-pyridyl 2-(3-pyrrolidinylcarbonyl)                                     142 H 3-pyridyl 2-glycinoyl                                                    143 H 3-pyridyl 2-(imidazol-1-ylacetyl)                                        144 H 2-pyrimidyl 2-(N-pyrrolidinyl-methyl)phenyl                              145 H 2-pyrimidyl 2-(N-piperidinyl-methyl)phenyl                               146 H 2-pyrimidyl 2-(N-morpholino-methyl)phenyl                                147 H 2-pyrimidyl 2-(N,N'-methylmorpholinium-                                     methyl)phenyl                                                               148 H 2-pyrimidyl 2-(N-pyridinium-methyl)phenyl                                149 H 2-pyrimidyl 2-(N-4-(N,N'-dimethylamino)-                                    pyridinium-methyl)phenyl                                                    150 H 2-pyrimidyl 2-(N-azatanyl-methyl)phenyl                                  151 H 2-pyrimidyl 2-(N-azetidinyl-methyl)phenyl                                152 H 2-pyrimidyl 2-(N-piperazinyl-methyl)phenyl                               153 H 2-pyrimidyl 2-(N,N'-BOC-piperazinyl-                                        methyl)phenyl                                                               154 H 2-pyrimidyl 2-(N-imidazolyl-methyl)phenyl                                155 H 2-pyrimidyl 2-(N-methoxy-N-methylamino-                                     methyl)phenyl                                                               156 H 2-pyrimidyl 2-(N-pyridonyl-methyl)phenyl                                 157 H 2-pyrimidyl 2-(N-(N',N'-dimethylhydrazinyl-                                 methyl)phenyl                                                               158 H 2-pyrimidyl 2-(amidinyl)phenyl                                           159 H 2-pyrimidyl 2-(N-guanidinyl)phenyl                                       160 H 2-pyrimidyl 2-(imidazolyl)phenyl                                         161 H 2-pyrimidyl 2-(imidazolidinyl)phenyl                                     162 H 2-pyrimidyl 2-(2-imidazolidinyl-                                            sulfonyl)phenyl                                                             163 H 2-pyrimidyl 2-(2-pyrrolidinyl)phenyl                                     164 H 2-pyrimidyl 2-(2-piperidinyl)phenyl                                      165 H 2-pyrimidyl 2-(amidinyl-methyl)phenyl                                    166 H 2-pyrimidyl 2-(2-imidazolidinyl-                                            methyl)phenyl                                                               167 H 2-pyrimidyl 2-(N-(2-aminoimidazolyl)-                                       methyl)phenyl                                                               168 H 2-pyrimidyl 2-dimethylaminoimidazol-1-yl                                 169 H 2-pyrimidyl 2-(3-aminophenyl)                                            170 H 2-pyrimidyl 2-(3-pyrrolidinylcarbonyl)                                   171 H 2-pyrimidyl 2-glycinoyl                                                  172 H 2-pyrimidyl 2-(imidazol-1-ylacetyl)                                      173 H 2-Cl-phenyl 2-(N-pyrrolidinyl-methyl)phenyl                              174 H 2-Cl-phenyl 2-(N-piperidinyl-methyl)phenyl                               175 H 2-Cl-phenyl 2-(N-morpholino-methyl)phenyl                                176 H 2-Cl-phenyl 2-(N,N'-methylmorpholinium-                                     methyl)phenyl                                                               177 H 2-Cl-phenyl 2-(N-pyridinium-methyl)phenyl                                178 H 2-Cl-phenyl 2-(N-4-(N,N'-dimethylamino)-                                    pyridinium-methyl)phenyl                                                    179 H 2-Cl-phenyl 2-(N-azatanyl-methyl)phenyl                                  180 H 2-Cl-phenyl 2-(N-azetidinyl-methyl)phenyl                                181 H 2-Cl-phenyl 2-(N-piperazinyl-methyl)phenyl                               182 H 2-Cl-phenyl 2-(N,N'-BOC-piperazinyl-                                        methyl)phenyl                                                               183 H 2-Cl-phenyl 2-(N-imidazolyl-methyl)phenyl                                184 H 2-Cl-phenyl 2-(N-methoxy-N-methylamino-                                     methyl)phenyl                                                               185 H 2-Cl-phenyl 2-(N-pyridonyl-methyl)phenyl                                 186 H 2-Cl-phenyl 2-(N-(N',N'-dimethylhydrazinyl-                                 methyl)phenyl                                                               187 H 2-Cl-phenyl 2-(amidinyl)phenyl                                           188 H 2-Cl-phenyl 2-(N-guanidinyl)phenyl                                       189 H 2-Cl-phenyl 2-(imidazolyl)phenyl                                         190 H 2-Cl-phenyl 2-(imidazolidinyl)phenyl                                     191 H 2-Cl-phenyl 2-(2-imidazolidinyl-                                            sulfonyl)phenyl                                                             192 H 2-Cl-phenyl 2-(2-pyrrolidinyl)phenyl                                     193 H 2-Cl-phenyl 2-(2-piperidinyl)phenyl                                      194 H 2-Cl-phenyl 2-(amidinyl-methyl)phenyl                                    195 H 2-Cl-phenyl 2-(2-imidazolidinyl-                                            methyl)phenyl                                                               196 H 2-Cl-phenyl 2-(N-(2-aminoimidazolyl)-                                       methyl)phenyl                                                               197 H 2-Cl-phenyl 2-dimethylaminoimidazol-1-yl                                 198 H 2-Cl-phenyl 2-(3-aminophenyl)                                            199 H 2-Cl-phenyl 2-(3-pyrrolidinylcarbonyl)                                   200 H 2-Cl-phenyl 2-glycinoyl                                                  201 H 2-Cl-phenyl 2-(imidazol-1-ylacetyl)                                      202 H 2-F-phenyl 2-(N-pyrrolidinyl-methyl)phenyl                               203 H 2-F-phenyl 2-(N-piperidinyl-methyl)phenyl                                204 H 2-F-phenyl 2-(N-morpholino-methyl)phenyl                                 205 H 2-F-phenyl 2-(N,N'-methylmorpholinium-                                      methyl)phenyl                                                               206 H 2-F-phenyl 2-(N-pyridinium-methyl)phenyl                                 207 H 2-F-phenyl 2-(N-4-(N,N'-dimethylamino)-                                     pyridinium-methyl)phenyl                                                    208 H 2-F-phenyl 2-(N-azatanyl-methyl)phenyl                                   209 H 2-F-phenyl 2-(N-azetidinyl-methyl)phenyl                                 210 H 2-F-phenyl 2-(N-piperazinyl-methyl)phenyl                                211 H 2-F-phenyl 2-(N,N'-BOC-piperazinyl-                                         methyl)phenyl                                                               212 H 2-F-phenyl 2-(N-imidazolyl-methyl)phenyl                                 213 H 2-F-phenyl 2-(N-methoxy-N-methylamino-                                      methyl)phenyl                                                               214 H 2-F-phenyl 2-(N-pyridonyl-methyl)phenyl                                  215 H 2-F-phenyl 2-(N-(N',N'-dimethylhydrazinyl-                                  methyl)phenyl                                                               216 H 2-F-phenyl 2-(amidinyl)phenyl                                            217 H 2-F-phenyl 2-(N-guanidinyl)phenyl                                        218 H 2-F-phenyl 2-(imidazolyl)phenyl                                          219 H 2-F-phenyl 2-(imidazolidinyl)phenyl                                      220 H 2-F-phenyl 2-(2-imidazolidinyl-                                             sulfonyl)phenyl                                                             221 H 2-F-phenyl 2-(2-pyrrolidinyl)phenyl                                      222 H 2-F-phenyl 2-(2-piperidinyl)phenyl                                       223 H 2-F-phenyl 2-(amidinyl-methyl)phenyl                                     224 H 2-F-phenyl 2-(2-imidazolidinyl-                                             methyl)phenyl                                                               225 H 2-F-phenyl 2-(N-(2-aminoimidazolyl)-                                        methyl)phenyl                                                               226 H 2-F-phenyl 2-dimethylaminoimidazol-1-yl                                  227 H 2-F-phenyl 2-(3-aminophenyl)                                             228 H 2-F-phenyl 2-(3-pyrrolidinylcarbonyl)                                    229 H 2-F-phenyl 2-glycinoyl                                                   230 H 2-F-phenyl 2-(imidazol-1-ylacetyl)                                       231 H 2,5-diF-phenyl 2-(N-pyrrolidinyl-methyl)phenyl                           232 H 2,5-diF-phenyl 2-(N-piperidinyl-methyl)phenyl                            233 H 2,5-diF-phenyl 2-(N-morpholino-methyl)phenyl                             234 H 2,5-diF-phenyl 2-(N,N'-methylmorpholinium-                                  methyl)phenyl                                                               235 H 2,5-diF-phenyl 2-(N-pyridinium-methyl)phenyl                             236 H 2,5-diF-phenyl 2-(N-4-(N,N'-dimethylamino)-                                 pyridinium-methyl)phenyl                                                    237 H 2,5-diF-phenyl 2-(N-azatanyl-methyl)phenyl                               238 H 2,5-diF-phenyl 2-(N-azetidinyl-methyl)phenyl                             239 H 2,5-diF-phenyl 2-(N-piperazinyl-methyl)phenyl                            240 H 2,5-diF-phenyl 2-(N,N'-BOC-piperazinyl-                                     methyl)phenyl                                                               241 H 2,5-diF-phenyl 2-(N-imidazolyl-methyl)phenyl                             242 H 2,5-diF-phenyl 2-(N-methoxy-N-methylamino-                                  methyl)phenyl                                                               243 H 2,5-diF-phenyl 2-(N-pyridonyl-methyl)phenyl                              244 H 2,5-diF-phenyl 2-(N-(N',N'-dimethylhydrazinyl-                              methyl)phenyl                                                               245 H 2,5-diF-phenyl 2-(amidinyl)phenyl                                        246 H 2,5-diF-phenyl 2-(N-guanidinyl)phenyl                                    247 H 2,5-diF-phenyl 2-(imidazolyl)phenyl                                      248 H 2,5-diF-phenyl 2-(imidazolidinyl)phenyl                                  249 H 2,5-diF-phenyl 2-(2-imidazolidinyl-                                         sulfonyl)phenyl                                                             250 H 2,5-diF-phenyl 2-(2-pyrrolidinyl)phenyl                                  251 H 2,5-diF-phenyl 2-(2-piperidinyl)phenyl                                   252 H 2,5-diF-phenyl 2-(amidinyl-methyl)phenyl                                 253 H 2,5-diF-phenyl 2-(2-imidazolidinyl-                                         methyl)phenyl                                                               254 H 2,5-diF-phenyl 2-(N-(2-aminoimidazolyl)-                                    methyl)phenyl                                                               255 H 2,5-diF-phenyl 2-dimethylaminoimidazol-1-yl                              256 H 2,5-diF-phenyl 2-(3-aminophenyl)                                         257 H 2,5-diF-phenyl 2-(3-pyrrolidinylcarbonyl)                                258 H 2,5-diF-phenyl 2-glycinoyl                                               259 H 2,5-diF-phenyl 2-(imidazol-1-ylacetyl)                                   260 --CN phenyl 2-(aminosulfonyl)phenyl                                        261 --CN phenyl 2-(methylaminosulfonyl)phenyl                                  262 --CN phenyl 1-pyrrolidinocarbonyl                                          263 --CN phenyl 2-(methylsulfonyl)phenyl                                       264 --CN phenyl 4-morpholino                                                   265 --CN phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                           266 --CN phenyl 4-morpholinocarbonyl                                           267 --CN 2-pyridyl 2-(aminosulfonyl)phenyl                                     268 --CN 2-pyridyl 2-(methylaminosulfonyl)phenyl                               269 --CN 2-pyridyl 1-pyrrolidinocarbonyl                                       270 --CN 2-pyridyl 2-(methylsulfonyl)phenyl                                    271 --CN 2-pyridyl 4-morpholino                                                272 --CN 2-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                        273 --CN 2-pyridyl 4-morpholinocarbonyl                                        274 --CN 3-pyridyl 2-(aminosulfonyl)phenyl                                     275 --CN 3-pyridyl 2-(methylaminosulfonyl)phenyl                               276 --CN 3-pyridyl 1-pyrrolidinocarbonyl                                       277 --CN 3-pyridyl 2-(methylsulfonyl)phenyl                                    278 --CN 3-pyridyl 4-morpholino                                                279 --CN 3-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                        280 --CN 3-pyridyl 4-morpholinocarbonyl                                        281 --CN 2-pyrimidyl 2-(aminosulfonyl)phenyl                                   282 --CN 2-pyrimidyl 2-(methylaminosulfonyl)phenyl                             283 --CN 2-pyrimidyl 1-pyrrolidinocarbonyl                                     284 --CN 2-pyrimidyl 2-(methylsulfonyl)phenyl                                  285 --CN 2-pyrimidyl 4-morpholino                                              286 --CN 2-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                      287 --CN 2-pyrimidyl 4-morpholinocarbonyl                                      288 --CN 5-pyrimidyl 2-(aminosulfonyl)phenyl                                   289 --CN 5-pyrimidyl 2-(methylaminosulfonyl)phenyl                             290 --CN 5-pyrimidyl 1-pyrrolidinocarbonyl                                     291 --CN 5-pyrimidyl 2-(methylsulfonyl)phenyl                                  292 --CN 5-pyrimidyl 4-morpholino                                              293 --CN 5-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                      294 --CN 5-pyrimidyl 4-morpholinocarbonyl                                      295 --CN 2-Cl-phenyl 2-(aminosulfonyl)phenyl                                   296 --CN 2-Cl-phenyl 2-(methylaminosulfonyl)phenyl                             297 --CN 2-Cl-phenyl 1-pyrrolidinocarbonyl                                     298 --CN 2-Cl-phenyl 2-(methylsulfonyl)phenyl                                  299 --CN 2-Cl-phenyl 4-morpholino                                              300 --CN 2-Cl-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                      301 --CN 2-Cl-phenyl 4-morpholinocarbonyl                                      302 --CN 2-F-phenyl 2-(aminosulfonyl)phenyl                                    303 --CN 2-F-phenyl 2-(methylaminosulfonyl)phenyl                              304 --CN 2-F-phenyl 1-pyrrolidinocarbonyl                                      305 --CN 2-F-phenyl 2-(methylsulfonyl)phenyl                                   306 --CN 2-F-phenyl 4-morpholino                                               307 --CN 2-F-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                       308 --CN 2-F-phenyl 4-morpholinocarbonyl                                       309 --CN 2,5-diF-phenyl 2-(aminosulfonyl)phenyl                                310 --CN 2,5-diF-phenyl 2-(methylaminosulfonyl)phenyl                          311 --CN 2,5-diF-phenyl 1-pyrrolidinocarbonyl                                  312 --CN 2,5-diF-phenyl 2-(methylsulfonyl)phenyl                               313 --CN 2,5-diF-phenyl 4-morpholino                                           314 --CN 2,5-diF-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                   315 --CN 2,5-diF-phenyl 4-morpholinocarbonyl                                   316 --CN phenyl 2-(N-pyrrolidinyl-methyl)phenyl                                317 --CN phenyl 2-(N-piperidinyl-methyl)phenyl                                 318 --CN phenyl 2-(N-morpholino-methyl)phenyl                                  319 --CN phenyl 2-(N,N'-methylmorpholinium-                                       methyl)phenyl                                                               320 --CN phenyl 2-(N-pyridinium-methyl)phenyl                                  321 --CN phenyl 2-(N-4-(N,N'-dimethylamino)-                                      pyridinium-methyl)phenyl                                                    322 --CN phenyl 2-(N-azatanyl-methyl)phenyl                                    323 --CN phenyl 2-(N-azetidinyl-methyl)phenyl                                  324 --CN phenyl 2-(N-piperazinyl-methyl)phenyl                                 325 --CN phenyl 2-(N,N'-BOC-piperazinyl-                                          methyl)phenyl                                                               326 --CN phenyl 2-(N-imidazolyl-methyl)phenyl                                  327 --CN phenyl 2-(N-methoxy-N-methylamino-                                       methyl)phenyl                                                               328 --CN phenyl 2-(N-pyridonyl-methyl)phenyl                                   329 --CN phenyl 2-(N-(N',N'-dimethylhydrazinyl-                                   methyl)phenyl                                                               330 --CN phenyl 2-(amidinyl)phenyl                                             331 --CN phenyl 2-(N-guanidinyl)phenyl                                         332 --CN phenyl 2-(imidazolyl)phenyl                                           333 --CN phenyl 2-(imidazolidinyl)phenyl                                       334 --CN phenyl 2-(2-imidazolidinyl-                                              sulfonyl)phenyl                                                             335 --CN phenyl 2-(2-pyrrolidinyl)phenyl                                       336 --CN phenyl 2-(2-piperidinyl)phenyl                                        337 --CN phenyl 2-(amidinyl-methyl)phenyl                                      338 --CN phenyl 2-(2-imidazolidinyl-                                              methyl)phenyl                                                               339 --CN phenyl 2-(N-(2-aminoimidazolyl)-                                         methyl)phenyl                                                               340 --CN phenyl 2-dimethylaminoimidazol-1-yl                                   341 --CN phenyl 2-(3-aminophenyl)                                              342 --CN phenyl 2-(3-pyrrolidinylcarbonyl)                                     343 --CN phenyl 2-glycinoyl                                                    344 --CN phenyl 2-(imidazol-1-ylacetyl)                                        345 --CN 2-pyridyl 2-(N-pyrrolidinyl-methyl)phenyl                             346 --CN 2-pyridyl 2-(N-piperidinyl-methyl)phenyl                              347 --CN 2-pyridyl 2-(N-morpholino-methyl)phenyl                               348 --CN 2-pyridyl 2-(N,N'-methylmorpholinium-                                    methyl)phenyl                                                               349 --CN 2-pyridyl 2-(N-pyridinium-methyl)phenyl                               350 --CN 2-pyridyl 2-(N-4-(N,N'-dimethylamino)-                                   pyridinium-methyl)phenyl                                                    351 --CN 2-pyridyl 2-(N-azatanyl-methyl)phenyl                                 352 --CN 2-pyridyl 2-(N-azetidinyl-methyl)phenyl                               353 --CN 2-pyridyl 2-(N-piperazinyl-methyl)phenyl                              354 --CN 2-pyridyl 2-(N,N'-BOC-piperazinyl-                                       methyl)phenyl                                                               355 --CN 2-pyridyl 2-(N-imidazolyl-methyl)phenyl                               356 --CN 2-pyridyl 2-(N-methoxy-N-methylamino-                                    methyl)phenyl                                                               357 --CN 2-pyridyl 2-(N-pyridonyl-methyl)phenyl                                358 --CN 2-pyridyl 2-(N-(N',N'-dimethylhydrazinyl-                                methyl)phenyl                                                               359 --CN 2-pyridyl 2-(amidinyl)phenyl                                          360 --CN 2-pyridyl 2-(N-guanidinyl)phenyl                                      361 --CN 2-pyridyl 2-(imidazolyl)phenyl                                        362 --CN 2-pyridyl 2-(imidazolidinyl)phenyl                                    363 --CN 2-pyridyl 2-(2-imidazolidinyl-                                           sulfonyl)phenyl                                                             364 --CN 2-pyridyl 2-(2-pyrrolidinyl)phenyl                                    365 --CN 2-pyridyl 2-(2-piperidinyl)phenyl                                     366 --CN 2-pyridyl 2-(amidinyl-methyl)phenyl                                   367 --CN 2-pyridyl 2-(2-imidazolidinyl-                                           methyl)phenyl                                                               368 --CN 2-pyridyl 2-(N-(2-aminoimidazolyl)-                                      methyl)phenyl                                                               369 --CN 2-pyridyl 2-dimethylaminoimidazol-1-yl                                370 --CN 2-pyridyl 2-(3-aminophenyl)                                           371 --CN 2-pyridyl 2-(3-pyrrolidinylcarbonyl)                                  372 --CN 2-pyridyl 2-glycinoyl                                                 373 --CN 2-pyridyl 2-(imidazol-1-ylacetyl)                                     374 --CN 3-pyridyl 2-(N-pyrrolidinyl-methyl)phenyl                             375 --CN 3-pyridyl 2-(N-piperidinyl-methyl)phenyl                              376 --CN 3-pyridyl 2-(N-morpholino-methyl)phenyl                               377 --CN 3-pyridyl 2-(N,N'-methylmorpholinium-                                    methyl)phenyl                                                               378 --CN 3-pyridyl 2-(N-pyridinium-methyl)phenyl                               379 --CN 3-pyridyl 2-(N-4-(N,N'-dimethylamino)-                                   pyridinium-methyl)phenyl                                                    380 --CN 3-pyridyl 2-(N-azatanyl-methyl)phenyl                                 381 --CN 3-pyridyl 2-(N-azetidinyl-methyl)phenyl                               382 --CN 3-pyridyl 2-(N-piperazinyl-methyl)phenyl                              383 --CN 3-pyridyl 2-(N,N'-BOC-piperazinyl-                                       methyl)phenyl                                                               384 --CN 3-pyridyl 2-(N-imidazolyl-methyl)phenyl                               385 --CN 3-pyridyl 2-(N-methoxy-N-methylamino-                                    methyl)phenyl                                                               386 --CN 3-pyridyl 2-(N-pyridonyl-methyl)phenyl                                387 --CN 3-pyridyl 2-(N-(N',N'-dimethylhydrazinyl-                                methyl)phenyl                                                               388 --CN 3-pyridyl 2-(amidinyl)phenyl                                          389 --CN 3-pyridyl 2-(N-guanidinyl)phenyl                                      390 --CN 3-pyridyl 2-(imidazolyl)phenyl                                        391 --CN 3-pyridyl 2-(imidazolidinyl)phenyl                                    392 --CN 3-pyridyl 2-(2-imidazolidinyl-                                           sulfonyl)phenyl                                                             393 --CN 3-pyridyl 2-(2-pyrrolidinyl)phenyl                                    394 --CN 3-pyridyl 2-(2-piperidinyl)phenyl                                     395 --CN 3-pyridyl 2-(amidinyl-methyl)phenyl                                   396 --CN 3-pyridyl 2-(2-imidazolidinyl-                                           methyl)phenyl                                                               397 --CN 3-pyridyl 2-(N-(2-aminoimidazolyl)-                                      methyl)phenyl                                                               398 --CN 3-pyridyl 2-dimethylaminoimidazol-1-yl                                399 --CN 3-pyridyl 2-(3-aminophenyl)                                           400 --CN 3-pyridyl 2-(3-pyrrolidinylcarbonyl)                                  401 --CN 3-pyridyl 2-glycinoyl                                                 402 --CN 3-pyridyl 2-(imidazol-1-ylacetyl)                                     403 --CN 2-pyrimidyl 2-(N-pyrrolidinyl-methyl)phenyl                           404 --CN 2-pyrimidyl 2-(N-piperidinyl-methyl)phenyl                            405 --CN 2-pyrimidyl 2-(N-morpholino-methyl)phenyl                             406 --CN 2-pyrimidyl 2-(N,N'-methylmorpholinium-                                  methyl)phenyl                                                               407 --CN 2-pyrimidyl 2-(N-pyridinium-methyl)phenyl                             408 --CN 2-pyrimidyl 2-(N-4-(N,N'-dimethylamino)-                                 pyridinium-methyl)phenyl                                                    409 --CN 2-pyrimidyl 2-(N-azatanyl-methyl)phenyl                               410 --CN 2-pyrimidyl 2-(N-azetidinyl-methyl)phenyl                             411 --CN 2-pyrimidyl 2-(N-piperazinyl-methyl)phenyl                            412 --CN 2-pyrimidyl 2-(N,N'-BOC-piperazinyl-                                     methyl)phenyl                                                               413 --CN 2-pyrimidyl 2-(N-imidazolyl-methyl)phenyl                             414 --CN 2-pyrimidyl 2-(N-methoxy-N-methylamino-                                  methyl)phenyl                                                               415 --CN 2-pyrimidyl 2-(N-pyridonyl-methyl)phenyl                              416 --CN 2-pyrimidyl 2-(N-(N',N'-dimethylhydrazinyl-                              methyl)phenyl                                                               417 --CN 2-pyrimidyl 2-(amidinyl)phenyl                                        418 --CN 2-pyrimidyl 2-(N-guanidinyl)phenyl                                    419 --CN 2-pyrimidyl 2-(imidazolyl)phenyl                                      420 --CN 2-pyrimidyl 2-(imidazolidinyl)phenyl                                  421 --CN 2-pyrimidyl 2-(2-imidazolidinyl-                                         sulfonyl)phenyl                                                             422 --CN 2-pyrimidyl 2-(2-pyrrolidinyl)phenyl                                  423 --CN 2-pyrimidyl 2-(2-piperidinyl)phenyl                                   424 --CN 2-pyrimidyl 2-(amidinyl-methyl)phenyl                                 425 --CN 2-pyrimidyl 2-(2-imidazolidinyl-                                         methyl)phenyl                                                               426 --CN 2-pyrimidyl 2-(N-(2-aminoimidazolyl)-                                    methyl)phenyl                                                               427 --CN 2-pyrimidyl 2-dimethylaminoimidazol-1-yl                              428 --CN 2-pyrimidyl 2-(3-aminophenyl)                                         429 --CN 2-pyrimidyl 2-(3-pyrrolidinylcarbonyl)                                430 --CN 2-pyrimidyl 2-glycinoyl                                               431 --CN 2-pyrimidyl 2-(imidazol-1-ylacetyl)                                   432 --CN 2-Cl-phenyl 2-(N-pyrrolidinyl-methyl)phenyl                           433 --CN 2-Cl-phenyl 2-(N-piperidinyl-methyl)phenyl                            434 --CN 2-Cl-phenyl 2-(N-morpholino-methyl)phenyl                             435 --CN 2-Cl-phenyl 2-(N,N'-methylmorpholinium-                                  methyl)phenyl                                                               436 --CN 2-Cl-phenyl 2-(N-pyridinium-methyl)phenyl                             437 --CN 2-Cl-phenyl 2-(N-4-(N,N'-dimethylamino)-                                 pyridinium-methyl)phenyl                                                    438 --CN 2-Cl-phenyl 2-(N-azatanyl-methyl)phenyl                               439 --CN 2-Cl-phenyl 2-(N-azetidinyl-methyl)phenyl                             440 --CN 2-Cl-phenyl 2-(N-piperazinyl-methyl)phenyl                            441 --CN 2-Cl-phenyl 2-(N,N'-BOC-piperazinyl-                                     methyl)phenyl                                                               442 --CN 2-Cl-phenyl 2-(N-imidazolyl-methyl)phenyl                             443 --CN 2-Cl-phenyl 2-(N-methoxy-N-methylamino-                                  methyl)phenyl                                                               444 --CN 2-Cl-phenyl 2-(N-pyridonyl-methyl)phenyl                              445 --CN 2-Cl-phenyl 2-(N-(N',N'-dimethylhydrazinyl-                              methyl)phenyl                                                               446 --CN 2-Cl-phenyl 2-(amidinyl)phenyl                                        447 --CN 2-Cl-phenyl 2-(N-guanidinyl)phenyl                                    448 --CN 2-Cl-phenyl 2-(imidazolyl)phenyl                                      449 --CN 2-Cl-phenyl 2-(imidazolidinyl)phenyl                                  450 --CN 2-Cl-phenyl 2-(2-imidazolidinyl-                                         sulfonyl)phenyl                                                             451 --CN 2-Cl-phenyl 2-(2-pyrrolidinyl)phenyl                                  452 --CN 2-Cl-phenyl 2-(2-piperidinyl)phenyl                                   453 --CN 2-Cl-phenyl 2-(amidinyl-methyl)phenyl                                 454 --CN 2-Cl-phenyl 2-(2-imidazolidinyl-                                         methyl)phenyl                                                               455 --CN 2-Cl-phenyl 2-(N-(2-aminoimidazolyl)-                                    methyl)phenyl                                                               456 --CN 2-Cl-phenyl 2-dimethylaminoimidazol-1-yl                              457 --CN 2-Cl-phenyl 2-(3-aminophenyl)                                         458 --CN 2-Cl-phenyl 2-(3-pyrrolidinylcarbonyl)                                459 --CN 2-Cl-phenyl 2-glycinoyl                                               460 --CN 2-Cl-phenyl 2-(imidazol-1-ylacetyl)                                   461 --CN 2-F-phenyl 2-(N-pyrrolidinyl-methyl)phenyl                            462 --CN 2-F-phenyl 2-(N-piperidinyl-methyl)phenyl                             463 --CN 2-F-phenyl 2-(N-morpholino-methyl)phenyl                              464 --CN 2-F-phenyl 2-(N,N'-methylmorpholinium-                                   methyl)phenyl                                                               465 --CN 2-F-phenyl 2-(N-pyridinium-methyl)phenyl                              466 --CN 2-F-phenyl 2-(N-4-(N,N'-dimethylamino)-                                  pyridinium-methyl)phenyl                                                    467 --CN 2-F-phenyl 2-(N-azatanyl-methyl)phenyl                                468 --CN 2-F-phenyl 2-(N-azetidinyl-methyl)phenyl                              469 --CN 2-F-phenyl 2-(N-piperazinyl-methyl)phenyl                             470 --CN 2-F-phenyl 2-(N,N'-BOC-piperazinyl-                                      methyl)phenyl                                                               471 --CN 2-F-phenyl 2-(N-imidazolyl-methyl)phenyl                              472 --CN 2-F-phenyl 2-(N-methoxy-N-methylamino-                                   methyl)phenyl                                                               473 --CN 2-F-phenyl 2-(N-pyridonyl-methyl)phenyl                               474 --CN 2-F-phenyl 2-(N-(N',N'-dimethylhydrazinyl-                               methyl)phenyl                                                               475 --CN 2-F-phenyl 2-(amidinyl)phenyl                                         476 --CN 2-F-phenyl 2-(N-guanidinyl)phenyl                                     477 --CN 2-F-phenyl 2-(imidazolyl)phenyl                                       478 --CN 2-F-phenyl 2-(imidazolidinyl)phenyl                                   479 --CN 2-F-phenyl 2-(2-imidazolidinyl-                                          sulfonyl)phenyl                                                             480 --CN 2-F-phenyl 2-(2-pyrrolidinyl)phenyl                                   481 --CN 2-F-phenyl 2-(2-piperidinyl)phenyl                                    482 --CN 2-F-phenyl 2-(amidinyl-methyl)phenyl                                  483 --CN 2-F-phenyl 2-(2-imidazolidinyl-                                          methyl)phenyl                                                               484 --CN 2-F-phenyl 2-(N-(2-aminoimidazolyl)-                                     methyl)phenyl                                                               485 --CN 2-F-phenyl 2-dimethylaminoimidazol-1-yl                               486 --CN 2-F-phenyl 2-(3-aminophenyl)                                          487 --CN 2-F-phenyl 2-(3-pyrrolidinylcarbonyl)                                 488 --CN 2-F-phenyl 2-glycinoyl                                                489 --CN 2-F-phenyl 2-(imidazol-1-ylacetyl)                                    490 --CN 2,5-diF-phenyl 2-(N-pyrrolidinyl-methyl)phenyl                        491 --CN 2,5-diF-phenyl 2-(N-piperidinyl-methyl)phenyl                         492 --CN 2,5-diF-phenyl 2-(N-morpholino-methyl)phenyl                          493 --CN 2,5-diF-phenyl 2-(N,N'-methylmorpholinium-                               methyl)phenyl                                                               494 --CN 2,5-diF-phenyl 2-(N-pyridinium-methyl)phenyl                          495 --CN 2,5-diF-phenyl 2-(N-4-(N,N'-dimethylamino)-                              pyridinium-methyl)phenyl                                                    496 --CN 2,5-diF-phenyl 2-(N-azatanyl-methyl)phenyl                            497 --CN 2,5-diF-phenyl 2-(N-azetidinyl-methyl)phenyl                          498 --CN 2,5-diF-phenyl 2-(N-piperazinyl-methyl)phenyl                         499 --CN 2,5-diF-phenyl 2-(N,N'-BOC-piperazinyl-                                  methyl)phenyl                                                               500 --CN 2,5-diF-phenyl 2-(N-imidazolyl-methyl)phenyl                          501 --CN 2,5-diF-phenyl 2-(N-methoxy-N-methylamino-                               methyl)phenyl                                                               502 --CN 2,5-diF-phenyl 2-(N-pyridonyl-methyl)phenyl                           503 --CN 2,5-diF-phenyl 2-(N-(N',N'-dimethylhydrazinyl-                           methyl)phenyl                                                               504 --CN 2,5-diF-phenyl 2-(amidinyl)phenyl                                     505 --CN 2,5-diF-phenyl 2-(N-guanidinyl)phenyl                                 506 --CN 2,5-diF-phenyl 2-(imidazolyl)phenyl                                   507 --CN 2,5-diF-phenyl 2-(imidazolidinyl)phenyl                               508 --CN 2,5-diF-phenyl 2-(2-imidazolidinyl-                                      sulfonyl)phenyl                                                             509 --CN 2,5-diF-phenyl 2-(2-pyrrolidinyl)phenyl                               510 --CN 2,5-diF-phenyl 2-(2-piperidinyl)phenyl                                511 --CN 2,5-diF-phenyl 2-(amidinyl-methyl)phenyl                              512 --CN 2,5-diF-phenyl 2-(2-imidazolidinyl-                                      methyl)phenyl                                                               513 --CN 2,5-diF-phenyl 2-(N-(2-aminoimidazolyl)-                                 methyl)phenyl                                                               514 --CN 2,5-diF-phenyl 2-dimethylaminoimidazol-1-yl                           515 --CN 2,5-diF-phenyl 2-(3-aminophenyl)                                      516 --CN 2,5-diF-phenyl 2-(3-pyrrolidinylcarbonyl)                             517 --CN 2,5-diF-phenyl 2-glycinoyl                                            518 --CN 2,5-diF-phenyl 2-(imidazol-1-ylacetyl)                                519 CF.sub.3  phenyl 2-(aminosulfonyl)phenyl                                   520 CF.sub.3  phenyl 2-(methylaminosulfonyl)phenyl                             521 CF.sub.3  phenyl 1-pyrrolidinocarbonyl                                     522 CF.sub.3  phenyl 2-(methylsulfonyl)phenyl                                  523 CF.sub.3  phenyl 4-morpholino                                              524 CF.sub.3  phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                      525 CF.sub.3  phenyl 4-morpholinocarbonyl                                      526 CF.sub.3  2-pyridyl 2-(aminosulfonyl)phenyl                                527 CF.sub.3  2-pyridyl 2-(methylaminosulfonyl)phenyl                          528 CF.sub.3  2-pyridyl 1-pyrrolidinocarbonyl                                  529 CF.sub.3  2-pyridyl 2-(methylsulfonyl)phenyl                               530 CF.sub.3  2-pyridyl 4-morpholino                                           531 CF.sub.3  2-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                   532 CF.sub.3  2-pyridyl 4-morpholinocarbonyl                                   533 CF.sub.3  3-pyridyl 2-(aminosulfonyl)phenyl                                534 CF.sub.3  3-pyridyl 2-(methylaminosulfonyl)phenyl                          535 CF.sub.3  3-pyridyl 1-pyrrolidinocarbonyl                                  536 CF.sub.3  3-pyridyl 2-(methylsulfonyl)phenyl                               537 CF.sub.3  3-pyridyl 4-morpholino                                           538 CF.sub.3  3-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                   539 CF.sub.3  3-pyridyl 4-morpholinocarbonyl                                   540 CF.sub.3  2-pyrimidyl 2-(aminosulfonyl)phenyl                              541 CF.sub.3  2-pyrimidyl 2-(methylaminosulfonyl)phenyl                        542 CF.sub.3  2-pyrimidyl 1-pyrrolidinocarbonyl                                543 CF.sub.3  2-pyrimidyl 2-(methylsulfonyl)phenyl                             544 CF.sub.3  2-pyrimidyl 4-morpholino                                         545 CF.sub.3  2-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                 546 CF.sub.3  2-pyrimidyl 4-morpholinocarbonyl                                 547 CF.sub.3  5-pyrimidyl 2-(aminosulfonyl)phenyl                              548 CF.sub.3  5-pyrimidyl 2-(methylaminosulfonyl)phenyl                        549 CF.sub.3  5-pyrimidyl 1-pyrrolidinocarbonyl                                550 CF.sub.3  5-pyrimidyl 2-(methylsulfonyl)phenyl                             551 CF.sub.3  5-pyrimidyl 4-morpholino                                         552 CF.sub.3  5-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                 553 CF.sub.3  5-pyrimidyl 4-morpholinocarbonyl                                 554 CF.sub.3  2-Cl-phenyl 2-(aminosulfonyl)phenyl                              555 CF.sub.3  2-Cl-phenyl 2-(methylaminosulfonyl)phenyl                        556 CF.sub.3  2-Cl-phenyl 1-pyrrolidinocarbonyl                                557 CF.sub.3  2-Cl-phenyl 2-(methylsulfonyl)phenyl                             558 CF.sub.3  2-Cl-phenyl 4-morpholino                                         559 CF.sub.3  2-Cl-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                 560 CF.sub.3  2-Cl-phenyl 4-morpholinocarbonyl                                 561 CF.sub.3  2-F-phenyl 2-(aminosulfonyl)phenyl                               562 CF.sub.3  2-F-phenyl 2-(methylaminosulfonyl)phenyl                         563 CF.sub.3  2-F-phenyl 1-pyrrolidinocarbonyl                                 564 CF.sub.3  2-F-phenyl 2-(methylsulfonyl)phenyl                              565 CF.sub.3  2-F-phenyl 4-morpholino                                          566 CF.sub.3  2-F-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                  567 CF.sub.3  2-F-phenyl 4-morpholinocarbonyl                                  568 CF.sub.3  2,5-diF-phenyl 2-(aminosulfonyl)phenyl                           569 CF.sub.3  2,5-diF-phenyl 2-(methylaminosulfonyl)phenyl                     570 CF.sub.3  2,5-diF-phenyl 1-pyrrolidinocarbonyl                             571 CF.sub.3  2,5-diF-phenyl 2-(methylsulfonyl)phenyl                          572 CF.sub.3  2,5-diF-phenyl 4-morpholino                                      573 CF.sub.3  2,5-diF-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                       574 CF.sub.3  2,5-diF-phenyl 4-morpholinocarbon                               yl                                                     575 CF.sub.3  phenyl 2-(N-pyrrolidinyl-methyl)phenyl                           576 CF.sub.3  phenyl 2-(N-piperidinyl-methyl)phenyl                            577 CF.sub.3  phenyl 2-(N-morpholino-methyl)phenyl                             578 CF.sub.3  phenyl 2-(N,N'-methylmorpholinium-                                  methyl)phenyl                                                               579 CF.sub.3  phenyl 2-(N-pyridinium-methyl)phenyl                             580 CF.sub.3  phenyl 2-(N-4-(N,N'-dimethylamino)-                                 pyridinium-methyl)phenyl                                                    581 CF.sub.3  phenyl 2-(N-azatanyl-methyl)phenyl                               582 CF.sub.3  phenyl 2-(N-azetidinyl-methyl)phenyl                             583 CF.sub.3  phenyl 2-(N-piperazinyl-methyl)phenyl                            584 CF.sub.3  phenyl 2-(N,N'-BOC-piperazinyl-                                     methyl)phenyl                                                               585 CF.sub.3  phenyl 2-(N-imidazolyl-methyl)phenyl                             586 CF.sub.3  phenyl 2-(N-methoxy-N-methylamino-                                  methyl)phenyl                                                               587 CF.sub.3  phenyl 2-(N-pyridonyl-methyl)phenyl                              588 CF.sub.3  phenyl 2-(N-(N',N'-dimethylhydrazinyl-                              methyl)phenyl                                                               589 CF.sub.3  phenyl 2-(amidinyl)phenyl                                        590 CF.sub.3  phenyl 2-(N-guanidinyl)phenyl                                    591 CF.sub.3  phenyl 2-(imidazolyl)phenyl                                      592 CF.sub.3  phenyl 2-(imidazolidinyl)phenyl                                  593 CF.sub.3  phenyl 2-(2-imidazolidinyl-                                         sulfonyl)phenyl                                                             594 CF.sub.3  phenyl 2-(2-pyrrolidinyl)phenyl                                  595 CF.sub.3  phenyl 2-(2-piperidinyl)phenyl                                   596 CF.sub.3  phenyl 2-(amidinyl-methyl)phenyl                                 597 CF.sub.3  phenyl 2-(2-imidazolidinyl-                                         methyl)phenyl                                                               598 CF.sub.3  phenyl 2-(N-(2-aminoimidazolyl)-                                    methyl)phenyl                                                               599 CF.sub.3  phenyl 2-dimethylaminoimidazol-1-yl                              600 CF.sub.3  phenyl 2-(3-aminophenyl)                                         601 CF.sub.3  phenyl 2-(3-pyrrolidinylcarbonyl)                                602 CF.sub.3  phenyl 2-glycinoyl                                               603 CF.sub.3  phenyl 2-(imidazol-1-ylacetyl)                                   604 CF.sub.3  2-pyridyl 2-(N-pyrrolidinyl-methyl)phenyl                        605 CF.sub.3  2-pyridyl 2-(N-piperidinyl-methyl)phenyl                         606 CF.sub.3  2-pyridyl 2-(N-morpholino-methyl)phenyl                          607 CF.sub.3  2-pyridyl 2-(N,N'-methylmorpholinium-                               methyl)phenyl                                                               608 CF.sub.3  2-pyridyl 2-(N-pyridinium-methyl)phenyl                          609 CF.sub.3  2-pyridyl 2-(N-4-(N,N'-dimethylamino)-                              pyridinium-methyl)phenyl                                                    610 CF.sub.3  2-pyridyl 2-(N-azatanyl-methyl)phenyl                            611 CF.sub.3  2-pyridyl 2-(N-azetidinyl-methyl)phenyl                          612 CF.sub.3  2-pyridyl 2-(N-piperazinyl-methyl)phenyl                         613 CF.sub.3  2-pyridyl 2-(N,N'-BOC-piperazinyl-                                  methyl)phenyl                                                               614 CF.sub.3  2-pyridyl 2-(N-imidazolyl-methyl)phenyl                          615 CF.sub.3  2-pyridyl 2-(N-methoxy-N-methylamino-                               methyl)phenyl                                                               616 CF.sub.3  2-pyridyl 2-(N-pyridonyl-methyl)phenyl                           617 CF.sub.3  2-pyridyl 2-(N-(N',N'-dimethylhydrazinyl-                           methyl)phenyl                                                               618 CF.sub.3  2-pyridyl 2-(amidinyl)phenyl                                     619 CF.sub.3  2-pyridyl 2-(N-guanidinyl)phenyl                                 620 CF.sub.3  2-pyridyl 2-(imidazolyl)phenyl                                   621 CF.sub.3  2-pyridyl 2-(imidazolidinyl)phenyl                               622 CF.sub.3  2-pyridyl 2-(2-imidazolidinyl-                                      sulfonyl)phenyl                                                             623 CF.sub.3  2-pyridyl 2-(2-pyrrolidinyl)phenyl                               624 CF.sub.3  2-pyridyl 2-(2-piperidinyl)phenyl                                625 CF.sub.3  2-pyridyl 2-(amidinyl-methyl)phenyl                              626 CF.sub.3  2-pyridyl 2-(2-imidazolidinyl-                                      methyl)phenyl                                                               627 CF.sub.3  2-pyridyl 2-(N-(2-aminoimidazolyl)-                                 methyl)phenyl                                                               628 CF.sub.3  2-pyridyl 2-dimethylaminoimidazol-1-yl                           629 CF.sub.3  2-pyridyl 2-(3-aminophenyl)                                      630 CF.sub.3  2-pyridyl 2-(3-pyrrolidinylcarbonyl)                             631 CF.sub.3  2-pyridyl 2-glycinoyl                                            632 CF.sub.3  2-pyridyl 2-(imidazol-1-ylacetyl)                                633 CF.sub.3  3-pyridyl 2-(N-pyrrolidinyl-methyl)phenyl                        634 CF.sub.3  3-pyridyl 2-(N-piperidinyl-methyl)phenyl                         635 CF.sub.3  3-pyridyl 2-(N-morpholino-methyl)phenyl                          636 CF.sub.3  3-pyridyl 2-(N,N'-methylmorpholinium-                               methyl)phenyl                                                               637 CF.sub.3  3-pyridyl 2-(N-pyridinium-methyl)phenyl                          638 CF.sub.3  3-pyridyl 2-(N-4-(N,N'-dimethylamino)-                              pyridinium-methyl)phenyl                                                    639 CF.sub.3  3-pyridyl 2-(N-azatanyl-methyl)phenyl                            640 CF.sub.3  3-pyridyl 2-(N-azetidinyl-methyl)phenyl                          641 CF.sub.3  3-pyridyl 2-(N-piperazinyl-methyl)phenyl                         642 CF.sub.3  3-pyridyl 2-(N,N'-BOC-piperazinyl-                                  methyl)phenyl                                                               643 CF.sub.3  3-pyridyl 2-(N-imidazolyl-methyl)phenyl                          644 CF.sub.3  3-pyridyl 2-(N-methoxy-N-methylamino-                               methyl)phenyl                                                               645 CF.sub.3  3-pyridyl 2-(N-pyridonyl-methyl)phenyl                           646 CF.sub.3  3-pyridyl 2-(N-(N',N'-dimethylhydrazinyl-                           methyl)phenyl                                                               647 CF.sub.3  3-pyridyl 2-(amidinyl)phenyl                                     648 CF.sub.3  3-pyridyl 2-(N-guanidinyl)phenyl                                 649 CF.sub.3  3-pyridyl 2-(imidazolyl)phenyl                                   650 CF.sub.3  3-pyridyl 2-(imidazolidinyl)phenyl                               651 CF.sub.3  3-pyridyl 2-(2-imidazolidinyl-                                      sulfonyl)phenyl                                                             652 CF.sub.3  3-pyridyl 2-(2-pyrrolidinyl)phenyl                               653 CF.sub.3  3-pyridyl 2-(2-piperidinyl)phenyl                                654 CF.sub.3  3-pyridyl 2-(amidinyl-methyl)phenyl                              655 CF.sub.3  3-pyridyl 2-(2-imidazolidinyl-                                      methyl)phenyl                                                               656 CF.sub.3  3-pyridyl 2-(N-(2-aminoimidazolyl)-                                 methyl)phenyl                                                               657 CF.sub.3  3-pyridyl 2-dimethylaminoimidazol-1-yl                           658 CF.sub.3  3-pyridyl 2-(3-aminophenyl)                                      659 CF.sub.3  3-pyridyl 2-(3-pyrrolidinylcarbonyl)                             660 CF.sub.3  3-pyridyl 2-glycinoyl                                            661 CF.sub.3  3-pyridyl 2-(imidazol-1-ylacetyl)                                662 CF.sub.3  2-pyrimidyl 2-(N-pyrrolidinyl-methyl)phenyl                      663 CF.sub.3  2-pyrimidyl 2-(N-piperidinyl-methyl)phenyl                       664 CF.sub.3  2-pyrimidyl 2-(N-morpholino-methyl)phenyl                        665 CF.sub.3  2-pyrimidyl 2-(N,N'-methylmorpholinium-                             methyl)phenyl                                                               666 CF.sub.3  2-pyrimidyl 2-(N-pyridinium-methyl)phenyl                        667 CF.sub.3  2-pyrimidyl 2-(N-4-(N,N'-dimethylamino)-                            pyridinium-methyl)phenyl                                                    668 CF.sub.3  2-pyrimidyl 2-(N-azatanyl-methyl)phenyl                          669 CF.sub.3  2-pyrimidyl 2-(N-azetidinyl-methyl)phenyl                        670 CF.sub.3  2-pyrimidyl 2-(N-piperazinyl-methyl)phenyl                       671 CF.sub.3  2-pyrimidyl 2-(N,N'-BOC-piperazinyl-                                methyl)phenyl                                                               672 CF.sub.3  2-pyrimidyl 2-(N-imidazolyl-methyl)phenyl                        673 CF.sub.3  2-pyrimidyl 2-(N-methoxy-N-methylamino-                             methyl)phenyl                                                               674 CF.sub.3  2-pyrimidyl 2-(N-pyridonyl-methyl)phenyl                         675 CF.sub.3  2-pyrimidyl 2-(N-(N',N'-dimethylhydrazinyl-                         methyl)phenyl                                                               676 CF.sub.3  2-pyrimidyl 2-(amidinyl)phenyl                                   677 CF.sub.3  2-pyrimidyl 2-(N-guanidinyl)phenyl                               678 CF.sub.3  2-pyrimidyl 2-(imidazolyl)phenyl                                 679 CF.sub.3  2-pyrimidyl 2-(imidazolidinyl)phenyl                             680 CF.sub.3  2-pyrimidyl 2-(2-imidazolidinyl-                                    sulfonyl)phenyl                                                             681 CF.sub.3  2-pyrimidyl 2-(2-pyrrolidinyl)phenyl                             682 CF.sub.3  2-pyrimidyl 2-(2-piperidinyl)phenyl                              683 CF.sub.3  2-pyrimidyl 2-(amidinyl-methyl)phenyl                            684 CF.sub.3  2-pyrimidyl 2-(2-imidazolidinyl-                                    methyl)phenyl                                                               685 CF.sub.3  2-pyrimidyl 2-(N-(2-aminoimidazolyl)-                               methyl)phenyl                                                               686 CF.sub.3  2-pyrimidyl 2-dimethylaminoimidazol-1-yl                         687 CF.sub.3  2-pyrimidyl 2-(3-aminophenyl)                                    688 CF.sub.3  2-pyrimidyl 2-(3-pyrrolidinylcarbonyl)                           689 CF.sub.3  2-pyrimidyl 2-glycinoyl                                          690 CF.sub.3  2-pyrimidyl 2-(imidazol-1-ylacetyl)                              691 CF.sub.3  2-Cl-phenyl 2-(N-pyrrolidinyl-methyl)phenyl                      692 CF.sub.3  2-Cl-phenyl 2-(N-piperidinyl-methyl)phenyl                       693 CF.sub.3  2-Cl-phenyl 2-(N-morpholino-methyl)phenyl                        694 CF.sub.3  2-Cl-phenyl 2-(N,N'-methylmorpholinium-                             methyl)phenyl                                                               695 CF.sub.3  2-Cl-phenyl 2-(N-pyridinium-methyl)phenyl                        696 CF.sub.3  2-Cl-phenyl 2-(N-4-(N,N'-dimethylamino)-                            pyridinium-methyl)phenyl                                                    697 CF.sub.3  2-Cl-phenyl 2-(N-azatanyl-methyl)phenyl                          698 CF.sub.3  2-Cl-phenyl 2-(N-azetidinyl-methyl)phenyl                        699 CF.sub.3  2-Cl-phenyl 2-(N-piperazinyl-methyl)phenyl                       700 CF.sub.3  2-Cl-phenyl 2-(N,N'-BOC-piperazinyl-                                methyl)phenyl                                                               701 CF.sub.3  2-Cl-phenyl 2-(N-imidazolyl-methyl)phenyl                        702 CF.sub.3  2-Cl-phenyl 2-(N-methoxy-N-methylamino-                             methyl)phenyl                                                               703 CF.sub.3  2-Cl-phenyl 2-(N-pyridonyl-methyl)phenyl                         704 CF.sub.3  2-Cl-phenyl 2-(N-(N',N'-dimethylhydrazinyl-                         methyl)phenyl                                                               705 CF.sub.3  2-Cl-phenyl 2-(amidinyl)phenyl                                   706 CF.sub.3  2-Cl-phenyl 2-(N-guanidinyl)phenyl                               707 CF.sub.3  2-Cl-phenyl 2-(imidazolyl)phenyl                                 708 CF.sub.3  2-Cl-phenyl 2-(imidazolidinyl)phenyl                             709 CF.sub.3  2-Cl-phenyl 2-(2-imidazolidinyl-                                    sultonyl)phenyl                                                             710 CF.sub.3  2-Cl-phenyl 2-(2-pyrrolidinyl)phenyl                             711 CF.sub.3  2-Cl-phenyl 2-(2-piperidinyl)phenyl                              712 CF.sub.3  2-Cl-phenyl 2-(amidinyl-methyl)phenyl                            713 CF.sub.3  2-Cl-phenyl 2-(2-imidazolidinyl-                                    methyl)phenyl                                                               714 CF.sub.3  2-Cl-phenyl 2-(N-(2-aminoimidazolyl)-                               methyl)phenyl                                                               715 CF.sub.3  2-Cl-phenyl 2-dimethylaminoimidazol-1-yl                         716 CF.sub.3  2-Cl-phenyl 2-(3-aminophenyl)                                    717 CF.sub.3  2-Cl-phenyl 2-(3-pyrrolidinylcarbonyl)                           718 CF.sub.3  2-Cl-phenyl 2-glycinoyl                                          719 CF.sub.3  2-Cl-phenyl 2-(imidazol-1-ylacetyl)                              720 CF.sub.3  2-F-phenyl 2-(N-pyrrolidinyl-methyl)phenyl                       721 CF.sub.3  2-F-phenyl 2-(N-piperidinyl-methyl)phenyl                        722 CF.sub.3  2-F-phenyl 2-(N-morpholino-methyl)phenyl                         723 CF.sub.3  2-F-phenyl 2-(N,N'-methylmorpholinium-                              methyl)phenyl                                                               724 CF.sub.3  2-F-phenyl 2-(N-pyridinium-methyl)phenyl                         725 CF.sub.3  2-F-phenyl 2-(N-4-(N,N'-dimethylamino)-                             pyridinium-methyl)phenyl                                                    726 CF.sub.3  2-F-phenyl 2-(N-azatanyl-methyl)phenyl                           727 CF.sub.3  2-F-phenyl 2-(N-azetidinyl-methyl)phenyl                         728 CF.sub.3  2-F-phenyl 2-(N-piperazinyl-methyl)phenyl                        729 CF.sub.3  2-F-phenyl 2-(N,N'-BOC-piperazinyl-                                 methyl)phenyl                                                               730 CF.sub.3  2-F-phenyl 2-(N-imidazolyl-methyl)phenyl                         731 CF.sub.3  2-F-phenyl 2-(N-methoxy-N-methylamino-                              methyl)phenyl                                                               732 CF.sub.3  2-F-phenyl 2-(N-pyridonyl-methyl)phenyl                          733 CF.sub.3  2-F-phenyl 2-(N-(N',N'-dimethylhydrazinyl-                          methyl)phenyl                                                               734 CF.sub.3  2-F-phenyl 2-(amidinyl)phenyl                                    735 CF.sub.3  2-F-phenyl 2-(N-guanidinyl)phenyl                                736 CF.sub.3  2-F-phenyl 2-(imidazolyl)phenyl                                  737 CF.sub.3  2-F-phenyl 2-(imidazolidinyl)phenyl                              738 CF.sub.3  2-F-phenyl 2-(2-imidazolidinyl-                                     sulfonyl)phenyl                                                             739 CF.sub.3  2-F-phenyl 2-(2-pyrrolidinyl)phenyl                              740 CF.sub.3  2-F-phenyl 2-(2-piperidinyl)phenyl                               741 CF.sub.3  2-F-phenyl 2-(amidinyl-methyl)phenyl                             742 CF.sub.3  2-F-phenyl 2-(2-imidazolidinyl-                                     methyl)phenyl                                                               743 CF.sub.3  2-F-phenyl 2-(N-(2-aminoimidazolyl)-                                methyl)phenyl                                                               744 CF.sub.3  2-F-phenyl 2-dimethylaminoimidazol-1-yl                          745 CF.sub.3  2-F-phenyl 2-(3-aminophenyl)                                     746 CF.sub.3  2-F-phenyl 2-(3-pyrrolidinylcarbonyl)                            747 CF.sub.3  2-F-phenyl 2-glycinoyl                                           748 CF.sub.3  2-F-phenyl 2-(imidazol-1-ylacetyl)                               749 CF.sub.3  2,5-diF-phenyl 2-(N-pyrrolidinyl-methyl)phenyl                   750 CF.sub.3  2,5-diF-phenyl 2-(N-piperidinyl-methyl)phenyl                    751 CF.sub.3  2,5-diF-phenyl 2-(N-morpholino-methyl)phenyl                     752 CF.sub.3  2,5-diF-phenyl 2-(N,N'-methylmorpholinium-                          methyl)phenyl                                                               753 CF.sub.3  2,5-diF-phenyl 2-(N-pyridinium-methyl)phenyl                     754 CF.sub.3  2,5-diF-phenyl 2-(N-4-(N,N'-dimethylamino)-                         pyridinium-methyl)phenyl                                                    755 CF.sub.3  2,5-diF-phenyl 2-(N-azatanyl-methyl)phenyl                       756 CF.sub.3  2,5-diF-phenyl 2-(N-azetidinyl-methyl)phenyl                     757 CF.sub.3  2,5-diF-phenyl 2-(N-piperazinyl-methyl)phenyl                    758 CF.sub.3  2,5-diF-phenyl 2-(N,N'-BOC-piperazinyl-                             methyl)phenyl                                                               759 CF.sub.3  2,5-diF-phenyl 2-(N-imidazolyl-methyl)phenyl                     760 CF.sub.3  2,5-diF-phenyl 2-(N-methoxy-N-methylamino-                          methyl)phenyl                                                               761 CF.sub.3  2,5-diF-phenyl 2-(N-pyridonyl-methyl)phenyl                      762 CF.sub.3  2,5-diF-phenyl 2-(N-(N',N'-dimethylhydrazinyl-                      methyl)phenyl                                                               763 CF.sub.3  2,5-diF-phenyl 2-(amidinyl)phenyl                                764 CF.sub.3  2,5-diF-phenyl 2-(N-guanidinyl)phenyl                            765 CF.sub.3  2,5-diF-phenyl 2-(imidazolyl)phenyl                              766 CF.sub.3  2,5-diF-phenyl 2-(imidazolidinyl)phenyl                          767 CF.sub.3  2,5-diF-phenyl 2-(2-imidazolidinyl-                                 sulfonyl)phenyl                                                             768 CF.sub.3  2,5-diF-phenyl 2-(2-pyrrolidinyl)phenyl                          769 CF.sub.3  2,5-diF-phenyl 2-(2-piperidinyl)phenyl                           770 CF.sub.3  2,5-diF-phenyl 2-(amidinyl-methyl)phenyl                         771 CF.sub.3  2,5-diF-phenyl 2-(2-imidazolidinyl-                                 methyl)phenyl                                                               772 CF.sub.3  2,5-diF-phenyl 2-(N-(2-aminoimidazolyl)-                            methyl)phenyl                                                               773 CF.sub.3  2,5-diF-phenyl 2-dimethylaminoimidazol-1-yl                      774 CF.sub.3  2,5-diF-phenyl 2-(3-aminophenyl)                                 775 CF.sub.3  2,5-diF-phenyl 2-(3-pyrrolidinylcarbonyl)                        776 CF.sub.3  2,5-diF-phenyl 2-glycinoyl                                       777 CF.sub.3  2,5-diF-phenyl 2-(imidazol-1-ylacetyl)                           778 CONH.sub.2 phenyl 2-(aminosulfonyl)phenyl                                  779 CONH.sub.2 phenyl 2-(methylaminosulfonyl)phenyl                            780 CONH.sub.2 phenyl 1-pyrrolidinocarbonyl                                    781 CONH.sub.2 phenyl 2-(methylsulfonyl)phenyl                                 782 CONH.sub.2 phenyl 4-morpholino                                             783 CONH.sub.2 phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                     784 CONH.sub.2 phenyl 4-morpholinocarbonyl                                     785 CONH.sub.2 2-pyridyl 2-(aminosulfonyl)phenyl                               786 CONH.sub.2 2-pyridyl 2-(methylaminosulfonyl)phenyl                         787 CONH.sub.2 2-pyridyl 1-pyrrolidinocarbonyl                                 788 CONH.sub.2 2-pyridyl 2-(methylsulfonyl)phenyl                              789 CONH.sub.2 2-pyridyl 4-morpholino                                          790 CONH.sub.2 2-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                  791 CONH.sub.2 2-pyridyl 4-morpholinocarbonyl                                  792 CONH.sub.2 3-pyridyl 2-(aminosulfonyl)phenyl                               793 CONH.sub.2 3-pyridyl 2-(methylaminosulfonyl)phenyl                         794 CONH.sub.2 3-pyridyl 1-pyrrolidinocarbonyl                                 795 CONH.sub.2 3-pyridyl 2-(methylsulfonyl)phenyl                              796 CONH.sub.2 3-pyridyl 4-morpholino                                          797 CONH.sub.2 3-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                  798 CONH.sub.2 3-pyridyl 4-morpholinocarbonyl                                  799 CONH.sub.2 2-pyrimidyl 2-(aminosulfonyl)phenyl                             800 CONH.sub.2 2-pyrimidyl 2-(methylaminosulfonyl)phenyl                       801 CONH.sub.2 2-pyrimidyl 1-pyrrolidinocarbonyl                               802 CONH.sub.2 2-pyrimidyl 2-(methylsulfonyl)phenyl                            803 CONH.sub.2 2-pyrimidyl 4-morpholino                                        804 CONH.sub.2 2-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                         805 CONH.sub.2 2-pyrimidyl 4-morpholinocarbonyl       806 CONH.sub.2 5-pyrimidyl 2-(aminosulfonyl)phenyl                             807 CONH.sub.2 5-pyrimidyl 2-(methylaminosulfonyl)phenyl                       808 CONH.sub.2 5-pyrimidyl 1-pyrrolidinocarbonyl                               809 CONH.sub.2 5-pyrimidyl 2-(methylsulfonyl)phenyl                            810 CONH.sub.2 5-pyrimidyl 4-morpholino                                        811 CONH.sub.2 5-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                         812 CONH.sub.2 5-pyrimidyl 4-morpholinocarbonyl       813 CONH.sub.2 2-Cl-phenyl 2-(aminosulfonyl)phenyl                             814 CONH.sub.2 2-Cl-phenyl 2-(methylaminosulfonyl)phenyl                       815 CONH.sub.2 2-Cl-phenyl 1-pyrrolidinocarbonyl                               816 CONH.sub.2 2-Cl-phenyl 2-(methylsulfonyl)phenyl                            817 CONH.sub.2 2-Cl-phenyl 4-morpholino                                        818 CONH.sub.2 2-Cl-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                         819 CONH.sub.2 2-Cl-phenyl 4-morpholinocarbonyl       820 CONH.sub.2 2-F-phenyl 2-(aminosulfonyl)phenyl                              821 CONH.sub.2 2-F-phenyl 2-(methylaminosulfonyl)phenyl                        822 CONH.sub.2 2-F-phenyl 1-pyrrolidinocarbonyl                                823 CONH.sub.2 2-F-phenyl 2-(methylsulfonyl)phenyl                             824 CONH.sub.2 2-F-phenyl 4-morpholino                                         825 CONH.sub.2 2-F-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                 826 CONH.sub.2 2-F-phenyl 4-morpholinocarbonyl                                 827 CONH.sub.2 2,5-diF-phenyl 2-(aminosulfonyl)phenyl                          828 CONH.sub.2 2,5-diF-phenyl 2-(methylaminosulfonyl)phenyl                    829 CONH.sub.2 2,5-diF-phenyl 1-pyrrolidinocarbonyl                            830 CONH.sub.2 2,5-diF-phenyl 2-(methylsulfonyl)phenyl                       831  CONH.sub.2                                                                               2,5-diF-phenyl                                                                            4-morpholino                                           832 CONH.sub.2 2,5-diF-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                      833 CONH.sub.2 2,5-diF-phenyl 4-morpholinocarbo                               nyl                                                    834 CONH.sub.2 phenyl 2-(N-pyrrolidinyl-methyl)phenyl                          835 CONH.sub.2 phenyl 2-(N-piperidinyl-methyl)phenyl                           836 CONH.sub.2 phenyl 2-(N-morpholino-methyl)phenyl                            837 CONH.sub.2 phenyl 2-(N,N'-methylmorpholinium-                                 methyl)phenyl                                                               838 CONH.sub.2 phenyl 2-(N-pyridinium-methyl)phenyl                            839 CONH.sub.2 phenyl 2-(N-4-(N,N'-dimethylamino)-                                pyridinium-methyl)phenyl                                                    840 CONH.sub.2 phenyl 2-(N-azatanyl-methyl)phenyl                              841 CONH.sub.2 phenyl 2-(N-azetidinyl-methyl)phenyl                            842 CONH.sub.2 phenyl 2-(N-piperazinyl-methyl)phenyl                           843 CONH.sub.2 phenyl 2-(N,N'-BOC-piperazinyl-                                    methyl)phenyl                                                               844 CONH.sub.2 phenyl 2-(N-imidazolyl-methyl)phenyl                            845 CONH.sub.2 phenyl 2-(N-methoxy-N-methylamino-                                 methyl)phenyl                                                               846 CONH.sub.2 phenyl 2-(N-pyridonyl-methyl)phenyl                             847 CONH.sub.2 phenyl 2-(N-(N',N'-dimethylhydrazinyl-                             methyl)phenyl                                                               848 CONH.sub.2 phenyl 2-(amidinyl)phenyl                                       849 CONH.sub.2 phenyl 2-(N-guanidinyl)phenyl                                   850 CONH.sub.2 phenyl 2-(imidazolyl)phenyl                                     851 CONH.sub.2 phenyl 2-(imidazolidinyl)phenyl                                 852 CONH.sub.2 phenyl 2-(2-imidazolidinyl-                                        sulfonyl)phenyl                                                             853 CONH.sub.2 phenyl 2-(2-pyrrolidinyl)phenyl                                 854 CONH.sub.2 phenyl 2-(2-piperidinyl)phenyl                                  855 CONH.sub.2 phenyl 2-(amidinyl-methyl)phenyl                                856 CONH.sub.2 phenyl 2-(2-imidazolidinyl-                                        methyl)phenyl                                                               857 CONH.sub.2 phenyl 2-(N-(2-aminoimidazolyl)-                                   methyl)phenyl                                                               858 CONH.sub.2 phenyl 2-dimethylaminoimidazol-1-yl                             859 CONH.sub.2 phenyl 2-(3-aminophenyl)                                        860 CONH.sub.2 phenyl 2-(3-pyrrolidinylcarbonyl)                               861 CONH.sub.2 phenyl 2-glycinoyl                                              862 CONH.sub.2 phenyl 2-(imidazol-1-ylacetyl)                                  863 CONH.sub.2 2-pyridyl 2-(N-pyrrolidinyl-methyl)phenyl                       864 CONH.sub.2 2-pyridyl 2-(N-piperidinyl-methyl)phenyl                        865 CONH.sub.2 2-pyridyl 2-(N-morpholino-methyl)phenyl                         866 CONH.sub.2 2-pyridyl 2-(N,N'-methylmorpholinium-                              methyl)phenyl                                                               867 CONH.sub.2 2-pyridyl 2-(N-pyridinium-methyl)phenyl                         868 CONH.sub.2 2-pyridyl 2-(N-4-(N,N'-dimethylamino)-                             pyridinium-methyl)phenyl                                                    869 CONH.sub.2 2-pyridyl 2-(N-azatanyl-methyl)phenyl                           870 CONH.sub.2 2-pyridyl 2-(N-azetidinyl-methyl)phenyl                         871 CONH.sub.2 2-pyridyl 2-(N-piperazinyl-methyl)phenyl                        872 CONH.sub.2 2-pyridyl 2-(N,N'-BOC-piperazinyl-                                 methyl)phenyl                                                               873 CONH.sub.2 2-pyridyl 2-(N-imidazolyl-methyl)phenyl                         874 CONH.sub.2 2-pyridyl 2-(N-methoxy-N-methylamino-                              methyl)phenyl                                                               875 CONH.sub.2 2-pyridyl 2-(N-pyridonyl-methyl)phenyl                          876 CONH.sub.2 2-pyridyl 2-(N-(N',N'-dimethylhydrazinyl-                          methyl)phenyl                                                               877 CONH.sub.2 2-pyridyl 2-(amidinyl)phenyl                                    878 CONH.sub.2 2-pyridyl 2-(N-guanidinyl)phenyl                                879 CONH.sub.2 2-pyridyl 2-(imidazolyl)phenyl                                  880 CONH.sub.2 2-pyridyl 2-(imidazolidinyl)phenyl                              881 CONH.sub.2 2-pyridyl 2-(2-imidazolidinyl-                                     sulfonyl)phenyl                                                             882 CONH.sub.2 2-pyridyl 2-(2-pyrrolidinyl)phenyl                              883 CONH.sub.2 2-pyridyl 2-(2-piperidinyl)phenyl                               884 CONH.sub.2 2-pyridyl 2-(amidinyl-methyl)phenyl                             885 CONH.sub.2 2-pyridyl 2-(2-imidazolidinyl-                                     methyl)phenyl                                                               886 CONH.sub.2 2-pyridyl 2-(N-(2-aminoimidazolyl)-                                methyl)phenyl                                                               887 CONH.sub.2 2-pyridyl 2-dimethylaminoimidazol-1-yl                          888 CONH.sub.2 2-pyridyl 2-(3-aminophenyl)                                     889 CONH.sub.2 2-pyridyl 2-(3-pyrrolidinylcarbonyl)                            890 CONH.sub.2 2-pyridyl 2-glycinoyl                                           891 CONH.sub.2 2-pyridyl 2-(imidazol-1-ylacetyl)                               892 CONH.sub.2 3-pyridyl 2-(N-pyrrolidinyl-methyl)phenyl                       893 CONH.sub.2 3-pyridyl 2-(N-piperidinyl-methyl)phenyl                        894 CONH.sub.2 3-pyridyl 2-(N-morpholino-methyl)phenyl                         895 CONH.sub.2 3-pyridyl 2-(N,N'-methylmorpholinium-                              methyl)phenyl                                                               896 CONH.sub.2 3-pyridyl 2-(N-pyridinium-methyl)phenyl                         897 CONH.sub.2 3-pyridyl 2-(N-4-(N,N'-dimethylamino)-                             pyridinium-methyl)phenyl                                                    898 CONH.sub.2 3-pyridyl 2-(N-azatanyl-methyl)phenyl                           899 CONH.sub.2 3-pyridyl 2-(N-azetidinyl-methyl)phenyl                         900 CONH.sub.2 3-pyridyl 2-(N-piperazinyl-methyl)phenyl                        901 CONH.sub.2 3-pyridyl 2-(N,N'-BOC-piperazinyl-                                 methyl)phenyl                                                               902 CONH.sub.2 3-pyridyl 2-(N-imidazolyl-methyl)phenyl                         903 CONH.sub.2 3-pyridyl 2-(N-methoxy-N-methylamino-                              methyl)phenyl                                                               904 CONH.sub.2 3-pyridyl 2-(N-pyridonyl-methyl)phenyl                          905 CONH.sub.2 3-pyridyl 2-(N-(N',N'-dimethylhydrazinyl-                          methyl)phenyl                                                               906 CONH.sub.2 3-pyridyl 2-(amidinyl)phenyl                                    907 CONH.sub.2 3-pyridyl 2-(N-guanidinyl)phenyl                                908 CONH.sub.2 3-pyridyl 2-(imidazolyl)phenyl                                  909 CONH.sub.2 3-pyridyl 2-(imidazolidinyl)phenyl                              910 CONH.sub.2 3-pyridyl 2-(2-imidazolidinyl-                                     sulfonyl)phenyl                                                             911 CONH.sub.2 3-pyridyl 2-(2-pyrrolidinyl)phenyl                              912 CONH.sub.2 3-pyridyl 2-(2-piperidinyl)phenyl                               913 CONH.sub.2 3-pyridyl 2-(amidinyl-methyl)phenyl                             914 CONH.sub.2 3-pyridyl 2-(2-imidazolidinyl-                                     methyl)phenyl                                                               915 CONH.sub.2 3-pyridyl 2-(N-(2-aminoimidazolyl)-                                methyl)phenyl                                                               916 CONH.sub.2 3-pyridyl 2-dimethylaminoimidazol-1-yl                          917 CONH.sub.2 3-pyridyl 2-(3-aminophenyl)                                     918 CONH.sub.2 3-pyridyl 2-(3-pyrrolidinylcarbonyl)                            919 CONH.sub.2 3-pyridyl 2-glycinoyl                                           920 CONH.sub.2 3-pyridyl 2-(imidazol-1-ylacetyl)                               921 CONH.sub.2 2-pyrimidyl 2-(N-pyrrolidinyl-methyl)phenyl                     922 CONH.sub.2 2-pyrimidyl 2-(N-piperidinyl-methyl)phenyl                      923 CONH.sub.2 2-pyrimidyl 2-(N-morpholino-methyl)phenyl                       924 CONH.sub.2 2-pyrimidyl 2-(N,N'-methylmorpholinium-                            methyl)phenyl                                                               925 CONH.sub.2 2-pyrimidyl 2-(N-pyridinium-methyl)phenyl                       926 CONH.sub.2 2-pyrimidyl 2-(N-4-(N,N'-dimethylamino)-                           pyridinium-methyl)phenyl                                                    927 CONH.sub.2 2-pyrimidyl 2-(N-azatanyl-methyl)phenyl                         928 CONH.sub.2 2-pyrimidyl 2-(N-azetidinyl-methyl)phenyl                       929 CONH.sub.2 2-pyrimidyl 2-(N-piperazinyl-methyl)phenyl                      930 CONH.sub.2 2-pyrimidyl 2-(N,N'-BOC-piperazinyl-                               methyl)phenyl                                                               931 CONH.sub.2 2-pyrimidyl 2-(N-imidazolyl-methyl)phenyl                       932 CONH.sub.2 2-pyrimidyl 2-(N-methoxy-N-methylamino-                            methyl)phenyl                                                               933 CONH.sub.2 2-pyrimidyl 2-(N-pyridonyl-methyl)phenyl                        934 CONH.sub.2 2-pyrimidyl 2-(N-(N',N'-dimethylhydrazinyl-                        methyl)phenyl                                                               935 CONH.sub.2 2-pyrimidyl 2-(amidinyl)phenyl                                  936 CONH.sub.2 2-pyrimidyl 2-(N-guanidinyl)phenyl                              937 CONH.sub.2 2-pyrimidyl 2-(imidazolyl)phenyl                                938 CONH.sub.2 2-pyrimidyl 2-(imidazolidinyl)phenyl                            939 CONH.sub.2 2-pyrimidyl 2-(2-imidazolidinyl-                                   sulfonyl)phenyl                                                             940 CONH.sub.2 2-pyrimidyl 2-(2-pyrrolidinyl)phenyl                            941 CONH.sub.2 2-pyrimidyl 2-(2-piperidinyl)phenyl                             942 CONH.sub.2 2-pyrimidyl 2-(amidinyl-methyl)phenyl                           943 CONH.sub.2 2-pyrimidyl 2-(2-imidazolidinyl-                                   methyl)phenyl                                                               944 CONH.sub.2 2-pyrimidyl 2-(N-(2-aminoimidazolyl)-                              methyl)phenyl                                                               945 CONH.sub.2 2-pyrimidyl 2-dimethylaminoimidazol-1-yl                        946 CONH.sub.2 2-pyrimidyl 2-(3-aminophenyl)                                   947 CONH.sub.2 2-pyrimidyl 2-(3-pyrrolidinylcarbonyl)                          948 CONH.sub.2 2-pyrimidyl 2-glycinoyl                                         949 CONH.sub.2 2-pyrimidyl 2-(imidazol-1-ylacetyl)                             950 CONH.sub.2 2-Cl-phenyl 2-(N-pyrrolidinyl-methyl)phenyl                     951 CONH.sub.2 2-Cl-phenyl 2-(N-piperidinyl-methyl)phenyl                      952 CONH.sub.2 2-Cl-phenyl 2-(N-morpholino-methyl)phenyl                       953 CONH.sub.2 2-Cl-phenyl 2-(N,N'-methylmorpholinium-                            methyl)phenyl                                                               954 CONH.sub.2 2-Cl-phenyl 2-(N-pyridinium-methyl)phenyl                       955 CONH.sub.2 2-Cl-phenyl 2-(N-4-(N,N'-dimethylamino)-                           pyridinium-methyl)phenyl                                                    956 CONH.sub.2 2-Cl-phenyl 2-(N-azatanyl-methyl)phenyl                         957 CONH.sub.2 2-Cl-phenyl 2-(N-azetidinyl-methyl)phenyl                       958 CONH.sub.2 2-Cl-phenyl 2-(N-piperazinyl-methyl)phenyl                      959 CONH.sub.2 2-Cl-phenyl 2-(N,N'-BOC-piperazinyl-                               methyl)phenyl                                                               960 CONH.sub.2 2-Cl-phenyl 2-(N-imidazolyl-methyl)phenyl                       961 CONH.sub.2 2-Cl-phenyl 2-(N-methoxy-N-methylamino-                            methyl)phenyl                                                               962 CONH.sub.2 2-Cl-phenyl 2-(N-pyridonyl-methyl)phenyl                        963 CONH.sub.2 2-Cl-phenyl 2-(N-(N',N'-dimethylhydrazinyl-                        methyl)phenyl                                                               964 CONH.sub.2 2-Cl-phenyl 2-(amidinyl)phenyl                                  965 CONH.sub.2 2-Cl-phenyl 2-(N-guanidinyl)phenyl                              966 CONH.sub.2 2-Cl-phenyl 2-(imidazolyl)phenyl                                967 CONH.sub.2 2-Cl-phenyl 2-(imidazolidinyl)phenyl                            968 CONH.sub.2 2-Cl-phenyl 2-(2-imidazolidinyl-                                   sulfonyl)phenyl                                                             969 CONH.sub.2 2-Cl-phenyl 2-(2-pyrrolidinyl)phenyl                            970 CONH.sub.2 2-Cl-phenyl 2-(2-piperidinyl)phenyl                             971 CONH.sub.2 2-Cl-phenyl 2-(amidinyl-methyl)phenyl                           972 CONH.sub.2 2-Cl-phenyl 2-(2-imidazolidinyl-                                   methyl)phenyl                                                               973 CONH.sub.2 2-Cl-phenyl 2-(N-(2-aminoimidazolyl)-                              methyl)phenyl                                                               974 CONH.sub.2 2-Cl-phenyl 2-dimethylaminoimidazol-1-yl                        975 CONH.sub.2 2-Cl-phenyl 2-(3-aminophenyl)                                   976 CONH.sub.2 2-Cl-phenyl 2-(3-pyrrolidinylcarbonyl)                          977 CONH.sub.2 2-Cl-phenyl 2-glycinoyl                                         978 CONH.sub.2 2-Cl-phenyl 2-(imidazol-1-ylacetyl)                             979 CONH.sub.2 2-F-phenyl 2-(N-pyrrolidinyl-methyl)phenyl                      980 CONH.sub.2 2-F-phenyl 2-(N-piperidinyl-methyl)phenyl                       981 CONH.sub.2 2-F-phenyl 2-(N-morpholino-methyl)phenyl                        982 CONH.sub.2 2-F-phenyl 2-(N,N'-methylmorpholinium-                             methyl)phenyl                                                               983 CONH.sub.2 2-F-phenyl 2-(N-pyridinium-methyl)phenyl                        984 CONH.sub.2 2-F-phenyl 2-(N-4-(N,N'-dimethylamino)-                            pyridinium-methyl)phenyl                                                    985 CONH.sub.2 2-F-phenyl 2-(N-azatanyl-methyl)phenyl                          986 CONH.sub.2 2-F-phenyl 2-(N-azetidinyl-methyl)phenyl                        987 CONH.sub.2 2-F-phenyl 2-(N-piperazinyl-methyl)phenyl                       988 CONH.sub.2 2-F-phenyl 2-(N,N'-BOC-piperazinyl-                                methyl)phenyl                                                               989 CONH.sub.2 2-F-phenyl 2-(N-imidazolyl-methyl)phenyl                        990 CONH.sub.2 2-F-phenyl 2-(N-methoxy-N-methylamino-                             methyl)phenyl                                                               991 CONH.sub.2 2-F-phenyl 2-(N-pyridonyl-methyl)phenyl                         992 CONH.sub.2 2-F-phenyl 2-(N-(N',N'-dimethylhydrazinyl-                         methyl)phenyl                                                               993 CONH.sub.2 2-F-phenyl 2-(amidinyl)phenyl                                   994 CONH.sub.2 2-F-phenyl 2-(N-guanidinyl)phenyl                               995 CONH.sub.2 2-F-phenyl 2-(imidazolyl)phenyl                                 996 CONH.sub.2 2-F-phenyl 2-(imidazolidinyl)phenyl                             997 CONH.sub.2 2-F-phenyl 2-(2-imidazolidinyl-                                    sulfonyl)phenyl                                                             998 CONH.sub.2 2-F-phenyl 2-(2-pyrrolidinyl)phenyl                             999 CONH.sub.2 2-F-phenyl 2-(2-piperidinyl)phenyl                              1000 CONH.sub.2 2-F-phenyl 2-(amidinyl-methyl)phenyl                           1001 CONH.sub.2 2-F-phenyl 2-(2-imidazolidinyl-                                   methyl)phenyl                                                               1002 CONH.sub.2 2-F-phenyl 2-(N-(2-aminoimidazolyl)-                              methyl)phenyl                                                               1003 CONH.sub.2 2-F-phenyl 2-dimethylaminoimidazol-1-yl                        1004 CONH.sub.2 2-F-phenyl 2-(3-aminophenyl)                                   1005 CONH.sub.2 2-F-phenyl 2-(3-pyrrolidinylcarbonyl)                          1006 CONH.sub.2 2-F-phenyl 2-glycinoyl                                         1007 CONH.sub.2 2-F-phenyl 2-(imidazol-1-ylacetyl)                             1008 CONH.sub.2 2,5-diF-phenyl 2-(N-pyrrolidinyl-methyl)phenyl                 1009 CONH.sub.2 2,5-diF-phenyl 2-(N-piperidinyl-methyl)phenyl                  1010 CONH.sub.2 2,5-diF-phenyl 2-(N-morpholino-methyl)phenyl                   1011 CONH.sub.2 2,5-diF-phenyl 2-(N,N'-methylmorpholinium-                        methyl)phenyl                                                               1012 CONH.sub.2 2,5-diF-phenyl 2-(N-pyridinium-methyl)phenyl                   1013 CONH.sub.2 2,5-diF-phenyl 2-(N-4-(N,N'-dimethylamino)-                       pyridinium-methyl)phenyl                                                    1014 CONH.sub.2 2,5-diF-phenyl 2-(N-azatanyl-methyl)phenyl                     1015 CONH.sub.2 2,5-diF-phenyl 2-(N-azetidinyl-methyl)phenyl                   1016 CONH.sub.2 2,5-diF-phenyl 2-(N-piperazinyl-methyl)phenyl                  1017 CONH.sub.2 2,5-diF-phenyl 2-(N,N'-BOC-piperazinyl-                           methyl)phenyl                                                               1018 CONH.sub.2 2,5-diF-phenyl 2-(N-imidazolyl-methyl)phenyl                   1019 CONH.sub.2 2,5-diF-phenyl 2-(N-methoxy-N-methylamino-                        methyl)phenyl                                                               1020 CONH.sub.2 2,5-diF-phenyl 2-(N-pyridonyl-methyl)phenyl                    1021 CONH.sub.2 2,5-diF-phenyl 2-(N-(N',N'-dimethylhydrazinyl-                    methyl)phenyl                                                               1022 CONH.sub.2 2,5-diF-phenyl 2-(amidinyl)phenyl                              1023 CONH.sub.2 2,5-diF-phenyl 2-(N-guanidinyl)phenyl                          1024 CONH.sub.2 2,5-diF-phenyl 2-(imidazolyl)phenyl                            1025 CONH.sub.2 2,5-diF-phenyl 2-(imidazolidinyl)phenyl                        1026 CONH.sub.2 2,5-diF-phenyl 2-(2-imidazolidinyl-                               sulfonyl)phenyl                                                             1027 CONH.sub.2 2,5-diF-phenyl 2-(2-pyrrolidinyl)phenyl                        1028 CONH.sub.2 2,5-diF-phenyl 2-(2-piperidinyl)phenyl                         1029 CONH.sub.2 2,5-diF-phenyl 2-(amidinyl-methyl)phenyl                       1030 CONH.sub.2 2,5-diF-phenyl 2-(2-imidazolidinyl-                               methyl)phenyl                                                               1031 CONH.sub.2 2,5-diF-phenyl 2-(N-(2-aminoimidazolyl)-                          methyl)phenyl                                                               1032 CONH.sub.2 2,5-diF-phenyl 2-dimethylaminoimidazol-1-yl                    1033 CONH.sub.2 2,5-diF-phenyl 2-(3-aminophenyl)                               1034 CONH.sub.2 2,5-diF-phenyl 2-(3-pyrrolidinylcarbonyl)                      1035 CONH.sub.2 2,5-diF-phenyl 2-glycinoyl                                     1036 CONH.sub.2 2,5-diF-phenyl 2-(imidazol-1-ylacetyl)                         1037 SCH.sub.3 phenyl 2-(aminosulfonyl)phenyl                                  1038 SCH.sub.3 phenyl 2-(methylaminosulfonyl)phenyl                            1039 SCH.sub.3 phenyl 1-pyrrolidinocarbonyl                                    1040 SCH.sub.3 phenyl 2-(methylsulfonyl)phenyl                                 1041 SCH.sub.3 phenyl 4-morpholino                                             1042 SCH.sub.3 phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                     1043 SCH.sub.3 phenyl 4-morpholinocarbonyl                                     1044 SCH.sub.3 2-pyridyl 2-(aminosulfonyl)phenyl                               1045 SCH.sub.3 2-pyridyl 2-(methylaminosulfonyl)phenyl                         1046 SCH.sub.3 2-pyridyl 1-pyrrolidinocarbonyl                                 1047 SCH.sub.3 2-pyridyl 2-(methylsulfonyl)phenyl                              1048 SCH.sub.3 2-pyridyl 4-morpholino                                          1049 SCH.sub.3 2-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                  1050 SCH.sub.3 2-pyridyl 4-morpholinocarbonyl                                  1051 SCH.sub.3 3-pyridyl 2-(aminosulfonyl)phenyl                               1052 SCH.sub.3 3-pyridyl 2-(methylaminosulfonyl)phenyl                         1053 SCH.sub.3 3-pyridyl 1-pyrrolidinocarbonyl                                 1054 SCH.sub.3 3-pyridyl 2-(methylsulfonyl)phenyl                              1055 SCH.sub.3 3-pyridyl 4-morpholino                                          1056 SCH.sub.3 3-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                  1057 SCH.sub.3 3-pyridyl 4-morpholinocarbonyl                                  1058 SCH.sub.3 2-pyrimidyl 2-(aminosulfonyl)phenyl                             1059 SCH.sub.3 2-pyrimidyl 2-(methylaminosulfonyl)phenyl                       1060 SCH.sub.3 2-pyrimidyl 1-pyrrolidinocarbonyl                               1061 SCH.sub.3 2-pyrimidyl 2-(methylsulfonyl)phenyl                            1062 SCH.sub.3 2-pyrimidyl 4-morpholino                                        1063 SCH.sub.3 2-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                         1064 SCH.sub.3 2-pyrimidyl 4-morpholinocarbonyl       1065 SCH.sub.3 5-pyrimidyl 2-(aminosulfonyl)phenyl                             1066 SCH.sub.3 5-pyrimidyl 2-(methylaminosulfonyl)phenyl                       1067 SCH.sub.3 5-pyrimidyl 1-pyrrolidinocarbonyl                               1068 SCH.sub.3 5-pyrimidyl 2-(methylsulfonyl)phenyl                            1069 SCH.sub.3 5-pyrimidyl 4-morpholino                                        1070 SCH.sub.3 5-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                         1071 SCH.sub.3 5-pyrimidyl 4-morpholinocarbonyl       1072 SCH.sub.3 2-Cl-phenyl 2-(aminosulfonyl)phenyl                             1073 SCH.sub.3 2-Cl-phenyl 2-(methylaminosulfonyl)phenyl                       1074 SCH.sub.3 2-Cl-phenyl 1-pyrrolidinocarbonyl                               1075 SCH.sub.3 2-Cl-phenyl 2-(methylsulfonyl)phenyl                            1076 SCH.sub.3 2-Cl-phenyl 4-morpholino                                        1077 SCH.sub.3 2-Cl-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                         1078 SCH.sub.3 2-Cl-phenyl 4-morpholinocarbonyl       1079 SCH.sub.3 2-F-phenyl 2-(aminosulfonyl)phenyl                              1080 SCH.sub.3 2-F-phenyl 2-(methylaminosulfonyl)phenyl                        1081 SCH.sub.3 2-F-phenyl 1-pyrrolidinocarbonyl                                1082 SCH.sub.3 2-F-phenyl 2-(methylsulfonyl)phenyl                             1083 SCH.sub.3 2-F-phenyl 4-morpholino                                         1084 SCH.sub.3 2-F-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                 1085 SCH.sub.3 2-F-phenyl 4-morpholinocarbonyl                                 1086 SCH.sub.3 2,5-diF-phenyl 2-(aminosulfonyl)phenyl                          1087 SCH.sub.3 2,5-diF-phenyl 2-(methylaminosulfonyl)phenyl                    1088 SCH.sub.3 2,5-diF-phenyl 1-pyrrolidinocarbonyl                            1089 SCH.sub.3 2,5-diF-phenyl 2-(methylsulfonyl)phenyl                         1090 SCH.sub.3 2,5-diF-phenyl 4-morpholino                                     1091 SCH.sub.3 2,5-diF-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                      1092 SCH.sub.3 2,5-diF-phenyl 4-morpholinocarbo                               nyl                                                    1093 SCH.sub.3 phenyl 2-(N-pyrrolidinyl-methyl)phenyl                          1094 SCH.sub.3 phenyl 2-(N-piperidinyl-methyl)phenyl                           1095 SCH.sub.3 phenyl 2-(N-morpholino-methyl)phenyl                            1096 SCH.sub.3 phenyl 2-(N,N'-methylmorpholinium-                                 methyl)phenyl                                                               1097 SCH.sub.3 phenyl 2-(N-pyridinium-methyl)phenyl                            1098 SCH.sub.3 phenyl 2-(N-4-(N,N'-dimethylamino)-                                pyridinium-methyl)phenyl                                                    1099 SCH.sub.3 phenyl 2-(N-azatanyl-methyl)phenyl                              1100 SCH.sub.3 phenyl 2-(N-azetidinyl-methyl)phenyl                            1101 SCH.sub.3 phenyl 2-(N-piperazinyl-methyl)phenyl                           1102 SCH.sub.3 phenyl 2-(N,N'-BOC-piperazinyl-                                    methyl)phenyl                                                               1103 SCH.sub.3 phenyl 2-(N-imidazolyl-methyl)phenyl                            1104 SCH.sub.3 phenyl 2-(N-methoxy-N-methylamino-                                 methyl)phenyl                                                               1105 SCH.sub.3 phenyl 2-(N-pyridonyl-methyl)phenyl                             1106 SCH.sub.3 phenyl 2-(N-(N',N'-dimethylhydrazinyl-                             methyl)phenyl                                                               1107 SCH.sub.3 phenyl 2-(amidinyl)phenyl                                       1108 SCH.sub.3 phenyl 2-(N-guanidinyl)phenyl                                   1109 SCH.sub.3 phenyl 2-(imidazolyl)phenyl                                     1110 SCH.sub.3 phenyl 2-(imidazolidinyl)phenyl                                 1111 SCH.sub.3 phenyl 2-(2-imidazolidinyl-                                        sulfonyl)phenyl                                                             1112 SCH.sub.3 phenyl 2-(2-pyrrolidinyl)phenyl                                 1113 SCH.sub.3 phenyl 2-(2-piperidinyl)phenyl                                  1114 SCH.sub.3 phenyl 2-(amidinyl-methyl)phenyl                                1115 SCH.sub.3 phenyl 2-(2-imidazolidinyl-                                        methyl)phenyl                                                               1116 SCH.sub.3 phenyl 2-(N-(2-aminoimidazolyl)-                                   methyl)phenyl                                                               1117 SCH.sub.3 phenyl 2-dimethylaminoimidazol-1-yl                             1118 SCH.sub.3 phenyl 2-(3-aminophenyl)                                        1119 SCH.sub.3 phenyl 2-(3-pyrrolidinylcarbonyl)                               1120 SCH.sub.3 phenyl 2-glycinoyl                                              1121 SCH.sub.3 phenyl 2-(imidazol-1-ylacetyl)                                  1122 SCH.sub.3 2-pyridyl 2-(N-pyrrolidinyl-methyl)phenyl                       1123 SCH.sub.3 2-pyridyl 2-(N-piperidinyl-methyl)phenyl                        1124 SCH.sub.3 2-pyridyl 2 (N-morpholino-methyl)phenyl                         1125 SCH.sub.3 2-pyridyl 2-(N,N'-methylmorpholinium-                              methyl)phenyl                                                               1126 SCH.sub.3 2-pyridyl 2-(N-pyridinium-methyl)phenyl                         1127 SCH.sub.3 2-pyridyl 2-(N-4-(N,N'-dimethylamino)-                             pyridinium-methyl)phenyl                                                    1128 SCH.sub.3 2-pyridyl 2-(N-azatanyl-methyl)phenyl                           1129 SCH.sub.3 2-pyridyl 2-(N-azetidinyl-methyl)phenyl                         1130 SCH.sub.3 2-pyridyl 2-(N-piperazinyl-methyl)phenyl                        1131 SCH.sub.3 2-pyridyl 2-(N,N'-BOC-piperazinyl-                                 methyl)phenyl                                                               1132 SCH.sub.3 2-pyridyl 2-(N-imidazolyl-methyl)phenyl                         1133 SCH.sub.3 2-pyridyl 2-(N-methoxy-N-methylamino-                              methyl)phenyl                                                               1134 SCH.sub.3 2-pyridyl 2-(N-pyridonyl-methyl)phenyl                          1135 SCH.sub.3 2-pyridyl 2-(N-(N',N'-dimethylhydrazinyl-                          methyl)phenyl                                                               1136 SCH.sub.3 2-pyridyl 2-(amidinyl)phenyl                                    1137 SCH.sub.3 2-pyridyl 2-(N-guanidinyl)phenyl                                1138 SCH.sub.3 2-pyridyl 2-(imidazolyl)phenyl                                  1139 SCH.sub.3 2-pyridyl 2-(imidazolidinyl)phenyl                              1140 SCH.sub.3 2-pyridyl 2-(2-imidazolidinyl-                                     sulfonyl)phenyl                                                             1141 SCH.sub.3 2-pyridyl 2-(2-pyrrolidinyl)phenyl                              1142 SCH.sub.3 2-pyridyl 2-(2-piperidinyl)phenyl                               1143 SCH.sub.3 2-pyridyl 2-(amidinyl-methyl)phenyl                             1144 SCH.sub.3 2-pyridyl 2-(2-imidazolidinyl-                                     methyl)phenyl                                                               1145 SCH.sub.3 2-pyridyl 2-(N-(2-aminoimidazolyl)-                                methyl)phenyl                                                               1146 SCH.sub.3 2-pyridyl 2-dimethylaminoimidazol-1-yl                          1147 SCH.sub.3 2-pyridyl 2-(3-aminophenyl)                                     1148 SCH.sub.3 2-pyridyl 2-(3-pyrrolidinylcarbonyl)                            1149 SCH.sub.3 2-pyridyl 2-glycinoyl                                           1150 SCH.sub.3 2-pyridyl 2-(imidazol-1-ylacetyl)                               1151 SCH.sub.3 3-pyridyl 2-(N-pyrrolidinyl-methyl)phenyl                       1152 SCH.sub.3 3-pyridyl 2-(N-piperidinyl-methyl)phenyl                        1153 SCH.sub.3 3-pyridyl 2-(N-morpholino-methyl)phenyl                         1154 SCH.sub.3 3-pyridyl 2-(N,N'-methylmorpholinium-                              methyl)phenyl                                                               1155 SCH.sub.3 3-pyridyl 2-(N-pyridinium-methyl)phenyl                         1156 SCH.sub.3 3-pyridyl 2-(N-4-(N,N'-dimethylamino)-                             pyridinium-methyl)phenyl                                                    1157 SCH.sub.3 3-pyridyl 2-(N-azatanyl-methyl)phenyl                           1158 SCH.sub.3 3-pyridyl 2-(N-azetidinyl-methyl)phenyl                         1159 SCH.sub.3 3-pyridyl 2-(N-piperazinyl-methyl)phenyl                        1160 SCH.sub.3 3-pyridyl 2-(N,N'-BOC-piperazinyl-                                 methyl)phenyl                                                               1161 SCH.sub.3 3-pyridyl 2-(N-imidazolyl-methyl)phenyl                         1162 SCH.sub.3 3-pyridyl 2-(N-methoxy-N-methylamino-                              methyl)phenyl                                                               1163 SCH.sub.3 3-pyridyl 2-(N-pyridonyl-methyl)phenyl                          1164 SCH.sub.3 3-pyridyl 2-(N-(N',N'-dimethylhydrazinyl-                          methyl)phenyl                                                               1165 SCH.sub.3 3-pyridyl 2-(amidinyl)phenyl                                    1166 SCH.sub.3 3-pyridyl 2-(N-guanidinyl)phenyl                                1167 SCH.sub.3 3-pyridyl 2-(imidazolyl)phenyl                                  1168 SCH.sub.3 3-pyridyl 2-(imidazolidinyl)phenyl                              1169 SCH.sub.3 3-pyridyl 2-(2-imidazolidinyl-                                     sulfonyl)phenyl                                                             1170 SCH.sub.3 3-pyridyl 2-(2-pyrrolidinyl)phenyl                              1171 SCH.sub.3 3-pyridyl 2-(2-piperidinyl)phenyl                               1172 SCH.sub.3 3-pyridyl 2-(amidinyl-methyl)phenyl                             1173 SCH.sub.3 3-pyridyl 2-(2-imidazolidinyl-                                     methyl)phenyl                                                               1174 SCH.sub.3 3-pyridyl 2-(N-(2-aminoimidazolyl)-                                methyl)phenyl                                                               1175 SCH.sub.3 3-pyridyl 2-dimethylaminoimidazol-1-yl                          1176 SCH.sub.3 3-pyridyl 2-(3-aminophenyl)                                     1177 SCH.sub.3 3-pyridyl 2-(3-pyrrolidinylcarbonyl)                            1178 SCH.sub.3 3-pyridyl 2-glycinoyl                                           1179 SCH.sub.3 3-pyridyl 2-(imidazol-1-ylacetyl)                               1180 SCH.sub.3 2-pyrimidyl 2-(N-pyrrolidinyl-methyl)phenyl                     1181 SCH.sub.3 2-pyrimidyl 2-(N-piperidinyl-methyl)phenyl                      1182 SCH.sub.3 2-pyrimidyl 2-(N-morpholino-methyl)phenyl                       1183 SCH.sub.3 2-pyrimidyl 2-(N,N'-methylmorpholinium-                            methyl)phenyl                                                               1184 SCH.sub.3 2-pyrimidyl 2-(N-pyridinium-methyl)phenyl                       1185 SCH.sub.3 2-pyrimidyl 2-(N-4-(N,N'-dimethylamino)-                           pyridinium-methyl)phenyl                                                    1186 SCH.sub.3 2-pyrimidyl 2-(N-azatanyl-methyl)phenyl                         1187 SCH.sub.3 2-pyrimidyl 2-(N-azetidinyl-methyl)phenyl                       1188 SCH.sub.3 2-pyrimidyl 2-(N-piperazinyl-methyl)phenyl                      1189 SCH.sub.3 2-pyrimidyl 2-(N,N'-BOC-piperazinyl-                               methyl)phenyl                                                               1190 SCH.sub.3 2-pyrimidyl 2-(N-imidazolyl-methyl)phenyl                       1191 SCH.sub.3 2-pyrimidyl 2-(N-methoxy-N-methylamino-                            methyl)phenyl                                                               1192 SCH.sub.3 2-pyrimidyl 2-(N-pyridonyl-methyl)phenyl                        1193 SCH.sub.3 2-pyrimidyl 2-(N-(N',N'-dimethylhydrazinyl-                        methyl)phenyl                                                               1194 SCH.sub.3 2-pyrimidyl 2-(amidinyl)phenyl                                  1195 SCH.sub.3 2-pyrimidyl 2-(N-guanidinyl)phenyl                              1196 SCH.sub.3 2-pyrimidyl 2-(imidazolyl)phenyl                                1197 SCH.sub.3 2-pyrimidyl 2-(imidazolidinyl)phenyl                            1198 SCH.sub.3 2-pyrimidyl 2-(2-imidazolidinyl-                                   sulfonyl)phenyl                                                             1199 SCH.sub.3 2-pyrinidyl 2-(2-pyrrolidinyl)phenyl                            1200 SCH.sub.3 2-pyrimidyl 2-(2-piperidinyl)phenyl                             1201 SCH.sub.3 2-pyrimidyl 2-(amidinyl-methyl)phenyl                           1202 SCH.sub.3 2-pyrimidyl 2-(2-imidazolidinyl-                                   methyl)phenyl                                                               1203 SCH.sub.3 2-pyrimidyl 2-(N-(2-aminoimidazolyl)-                              methyl)phenyl                                                               1204 SCH.sub.3 2-pyrimidyl 2-dimethylaminoimidazol-1-yl                        1205 SCH.sub.3 2-pyrimidyl 2-(3-aminophenyl)                                   1206 SCH.sub.3 2-pyrimidyl 2-(3-pyrrolidinylcarbonyl)                          1207 SCH.sub.3 2-pyrimidyl 2-glycinoyl                                         1208 SCH.sub.3 2-pyrimidyl 2-(imidazol-1-ylacetyl)                             1209 SCH.sub.3 2-Cl-phenyl 2-(N-pyrrolidinyl-methyl)phenyl                     1210 SCH.sub.3 2-Cl-phenyl 2-(N-piperidinyl-methyl)phenyl                      1211 SCH.sub.3 2-Cl-phenyl 2-(N-morpholino-methyl)phenyl                       1212 SCH.sub.3 2-Cl-phenyl 2-(N,N'-methylmorpholinium-                            methyl)phenyl                                                               1213 SCH.sub.3 2-Cl-phenyl 2-(N-pyridinium-methyl)phenyl                       1214 SCH.sub.3 2-Cl-phenyl 2-(N-4-(N,N'-dimethylamino)-                           pyridinium-methyl)phenyl                                                    1215 SCH.sub.3 2-Cl-phenyl 2-(N-azatanyl-methyl)phenyl                         1216 SCH.sub.3 2-Cl-phenyl 2-(N-azetidinyl-methyl)phenyl                       1217 SCH.sub.3 2-Cl-phenyl 2-(N-piperazinyl-methyl)phenyl                      1218 SCH.sub.3 2-Cl-phenyl 2-(N,N'-BOC-piperazinyl-                               methyl)phenyl                                                               1219 SCH.sub.3 2-Cl-phenyl 2-(N-imidazolyl-methyl)phenyl                       1220 SCH.sub.3 2-Cl-phenyl 2-(N-methoxy-N-methylamino-                            methyl)phenyl                                                               1221 SCH.sub.3 2-Cl-phenyl 2-(N-pyridonyl-methyl)phenyl                        1222 SCH.sub.3 2-Cl-phenyl 2-(N-(N',N'-dimethylhydrazinyl-                        methyl)phenyl                                                               1223 SCH.sub.3 2-Cl-phenyl 2-(amidinyl)phenyl                                  1224 SCH.sub.3 2-Cl-phenyl 2-(N-guanidinyl)phenyl                              1225 SCH.sub.3 2-Cl-phenyl 2-(imidazolyl)phenyl                                1226 SCH.sub.3 2-Cl-phenyl 2-(imidazolidinyl)phenyl                            1227 SCH.sub.3 2-Cl-phenyl 2-(2-imidazolidinyl-                                   sulfonyl)phenyl                                                             1228 SCH.sub.3 2-Cl-phenyl 2-(2-pyrrolidinyl)phenyl                            1229 SCH.sub.3 2-Cl-phenyl 2-(2-piperidinyl)phenyl                             1230 SCH.sub.3 2-Cl-phenyl 2-(amidinyl-methyl)phenyl                           1231 SCH.sub.3 2-Cl-phenyl 2-(2-imidazolidinyl-                                   methyl)phenyl                                                               1232 SCH.sub.3 2-Cl-phenyl 2-(N-(2-aminoimidazolyl)-                              methyl)phenyl                                                               1233 SCH.sub.3 2-Cl-phenyl 2-dimethylaminoimidazol-1-yl                        1234 SCH.sub.3 2-Cl-phenyl 2-(3-aminophenyl)                                   1235 SCH.sub.3 2-Cl-phenyl 2-(3-pyrrolidinylcarbonyl)                          1236 SCH.sub.3 2-Cl-phenyl 2-glycinoyl                                         1237 SCH.sub.3 2-Cl-phenyl 2-(imidazol-1-ylacetyl)                             1238 SCH.sub.3 2-F-phenyl 2-(N-pyrrolidinyl-methyl)phenyl                      1239 SCH.sub.3 2-F-phenyl 2-(N-piperidinyl-methyl)phenyl                       1240 SCH.sub.3 2-F-phenyl 2-(N-morpholino-methyl)phenyl                        1241 SCH.sub.3 2-F-phenyl 2-(N,N'-methylmorpholinium-                             methyl)phenyl                                                               1242 SCH.sub.3 2-F-phenyl 2-(N-pyridinium-methyl)phenyl                        1243 SCH.sub.3 2-F-phenyl 2-(N-4-(N,N'-dimethylamino)-                            pyridinium-methyl)phenyl                                                    1244 SCH.sub.3 2-F-phenyl 2-(N-azatanyl-methyl)phenyl                          1245 SCH.sub.3 2-F-phenyl 2-(N-azetidinyl-methyl)phenyl                        1246 SCH.sub.3 2-F-phenyl 2-(N-piperazinyl-methyl)phenyl                       1247 SCH.sub.3 2-F-phenyl 2-(N,N'-BOC-piperazinyl-                                methyl)phenyl                                                               1248 SCH.sub.3 2-F-phenyl 2-(N-imidazolyl-methyl)phenyl                        1249 SCH.sub.3 2-F-phenyl 2-(N-methoxy-N-methylamino-                             methyl)phenyl                                                               1250 SCH.sub.3 2-F-phenyl 2-(N-pyridonyl-methyl)phenyl                         1251 SCH.sub.3 2-F-phenyl 2-(N-(N',N'-dimethylhydrazinyl                          methyl)phenyl                                                               1252 SCH.sub.3 2-F-phenyl 2-(amidinyl)phenyl                                   1253 SCH.sub.3 2-F-phenyl 2-(N-guanidinyl)phenyl                               1254 SCH.sub.3 2-F-phenyl 2-(imidazolyl)phenyl                                 1255 SCH.sub.3 2-F-phenyl 2-(imidazolidinyl)phenyl                             1256 SCH.sub.3 2-F-phenyl 2-(2-imidazolidinyl-                                    sulfonyl)phenyl                                                             1257 SCH.sub.3 2-F-phenyl 2-(2-pyrrolidinyl)phenyl                             1258 SCH.sub.3 2-F-phenyl 2-(2-piperidinyl)phenyl                              1259 SCH.sub.3 2-F-phenyl 2-(amidinyl-methyl)phenyl                            1260 SCH.sub.3 2-F-phenyl 2-(2-imidazolidinyl-                                    methyl)phenyl                                                               1261 SCH.sub.3 2-F-phenyl 2-(N-(2-aminoimidazolyl)-                               methyl)phenyl                                                               1262 SCH.sub.3 2-F-phenyl 2-dimethylaminoimidazol-1-yl                         1263 SCH.sub.3 2-F-phenyl 2-(3-aminophenyl)                                    1264 SCH.sub.3 2-F-phenyl 2-(3-pyrrolidinylcarbonyl)                           1265 SCH.sub.3 2-F-phenyl 2-glycinoyl                                          1266 SCH.sub.3 2-F-phenyl 2-(imidazol-1-ylacetyl)                              1267 SCH.sub.3 2,5-diF-phenyl 2-(N-pyrrolidinyl-methyl)phenyl                  1268 SCH.sub.3 2,5-diF-phenyl 2-(N-piperidinyl-methyl)phenyl                   1269 SCH.sub.3 2,5-diF-phenyl 2-(N-morpholino-methyl)phenyl                    1270 SCH.sub.3 2,5-diF-phenyl 2-(N,N'-methylmorpholinium-                         methyl)phenyl                                                               1271 SCH.sub.3 2,5-diF-phenyl 2-(N-pyridinium-methyl)phenyl                    1272 SCH.sub.3 2,5-diF-phenyl 2-(N-4-(N,N'-dimethylamino)-                        pyridinium-methyl)phenyl                                                    1273 SCH.sub.3 2,5-diF-phenyl 2-(N-azatanyl-methyl)phenyl                      1274 SCH.sub.3 2,5-diF-phenyl 2-(N-azetidinyl-methyl)phenyl                    1275 SCH.sub.3 2,5-diF-phenyl 2-(N-piperazinyl-methyl)phenyl                   1276 SCH.sub.3 2,5-diF-phenyl 2-(N,N'-BOC-piperazinyl-                            methyl)phenyl                                                               1277 SCH.sub.3 2,5-diF-phenyl 2-(N-imidazolyl-methyl)phenyl                    1278 SCH.sub.3 2,5-diF-phenyl 2-(N-methoxy-N-methylamino-                         methyl)phenyl                                                               1279 SCH.sub.3 2,5-diF-phenyl 2-(N-pyridonyl-methyl)phenyl                     1280 SCH.sub.3 2,5-diF-phenyl 2-(N-(N',N'-dimethylhydrazinyl-                     methyl)phenyl                                                               1281 SCH.sub.3 2,5-diF-phenyl 2-(amidinyl)phenyl                               1282 SCH.sub.3 2,5-diF-phenyl 2-(N-guanidinyl)phenyl                           1283 SCH.sub.3 2,5-diF-phenyl 2-(imidazolyl)phenyl                             1284 SCH.sub.3 2,5-diF-phenyl 2-(imidazolidinyl)phenyl                         1285 SCH.sub.3 2,5-diF-phenyl 2-(2-imidazolidinyl-                                sulfonyl)phenyl                                                             1286 SCH.sub.3 2,5-diF-phenyl 2-(2-pyrrolidinyl)phenyl                         1287 SCH.sub.3 2,5-diF-phenyl 2-(2-piperidinyl)phenyl                          1288 SCH.sub.3 2,5-diF-phenyl 2-(amidinyl-methyl)phenyl                        1289 SCH.sub.3 2,5-diF-phenyl 2-(2-imidazolidinyl-                                methyl)phenyl                                                               1290 SCH.sub.3 2,5-diF-phenyl 2-(N-(2-aminoimidazolyl)-                           methyl)phenyl                                                               1291 SCH.sub.3 2,5-diF-phenyl 2-dimethylaminoimidazol-1-yl                     1292 SCH.sub.3 2,5-diF-phenyl 2-(3-aminophenyl)                                1293 SCH.sub.3 2,5-diF-phenyl 2-(3-pyrrolidinylcarbonyl)                       1294 SCH.sub.3 2,5-diF-phenyl 2-glycinoyl                                      1295 SCH.sub.3 2,5-diF-phenyl 2-(imidazol-1-ylacetyl)                          1296 SO.sub.2 CH.sub.3 phenyl 2-(aminosulfonyl)phenyl                          1297 SO.sub.2 CH.sub.3 phenyl 2-(methylaminosulfonyl)phenyl                    1298 SO.sub.2 CH.sub.3 phenyl 1-pyrrolidinocarbonyl                            1299 SO.sub.2 CH.sub.3 phenyl 2-(methylsulfonyl)phenyl                         1300 SO.sub.2 CH.sub.3 phenyl 4-morpholino                                     1301 SO.sub.2 CH.sub.3 phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                      1302 SO.sub.2 CH.sub.3 phenyl 4-morpholinocarbo                               nyl                                                    1303 SO.sub.2 CH.sub.3 2-pyridyl 2-(aminosulfonyl)phenyl                       1304 SO.sub.2 CH.sub.3 2-pyridyl 2-(methylaminosulfonyl)phenyl                 1305 SO.sub.2 CH.sub.3 2-pyridyl 1-pyrrolidinocarbonyl                         1306 SO.sub.2 CH.sub.3 2-pyridyl 2-(methylsulfonyl)phenyl                      1307 SO.sub.2 CH.sub.3 2-pyridyl 4-morpholino                                  1308 SO.sub.2 CH.sub.3 2-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                   1309 SO.sub.2 CH.sub.3 2-pyridyl 4-morpholinoca                               rbonyl                                                 1310 SO.sub.2 CH.sub.3 3-pyridyl 2-(aminosulfonyl)phenyl                       1311 SO.sub.2 CH.sub.3 3-pyridyl 2-(methylaminosulfonyl)phenyl                 1312 SO.sub.2 CH.sub.3 3-pyridyl 1-pyrrolidinocarbonyl                         1313 SO.sub.2 CH.sub.3 3-pyridyl 2-(methylsulfonyl)phenyl                      1314 SO.sub.2 CH.sub.3 3-pyridyl 4-morpholino                                  1315 SO.sub.2 CH.sub.3 3-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                   1316 SO.sub.2 CH.sub.3 3-pyridyl 4-morpholinoca                               rbonyl                                                 1317 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(aminosulfonyl)phenyl                     1318 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(methylaminosulfonyl)phenyl                                        1319 SO.sub.2 CH.sub.3 2-pyrimidyl 1-pyrrolidin                               ocarbonyl                                              1320 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(methylsulfonyl)phenyl                    1321 SO.sub.2 CH.sub.3 2-pyrimidyl 4-morpholino                                1322 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl        1323 SO.sub.2 CH.sub.3 2-pyrimidyl 4-morpholinocarbonyl                        1324 SO.sub.2 CH.sub.3 5-pyrimidyl 2-(aminosulfonyl)phenyl                     1325 SO.sub.2 CH.sub.3 5-pyrimidyl 2-(methylaminosulfonyl)phenyl                                        1326 SO.sub.2 CH.sub.3 5-pyrimidyl 1-pyrrolidin                               ocarbonyl                                              1327 SO.sub.2 CH.sub.3 5-pyrimidyl 2-(methylsulfonyl)phenyl                    1328 SO.sub.2 CH.sub.3 5-pyrimidyl 4-morpholino                                1329 SO.sub.2 CH.sub.3 5-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl        1330 SO.sub.2 CH.sub.3 5-pyrimidyl 4-morpholinocarbonyl                        1331 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(aminosulfonyl)phenyl                     1332 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(methylaminosulfonyl)phenyl                                        1333 SO.sub.2 CH.sub.3 2-Cl-phenyl 1-pyrrolidin                               ocarbonyl                                              1334 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(methylsulfonyl)phenyl                    1335 SO.sub.2 CH.sub.3 2-Cl-phenyl 4-morpholino                                1336 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl        1337 SO.sub.2 CH.sub.3 2-Cl-phenyl 4-morpholinocarbonyl                        1338 SO.sub.2 CH.sub.3 2-F-phenyl 2-(aminosulfonyl)phenyl                      1339 SO.sub.2 CH.sub.3 2-F-phenyl 2-(methylaminosulfonyl)phenyl                                         1340 SO.sub.2 CH.sub.3 2-F-phenyl 1-pyrrolidino                               carbonyl                                               1341 SO.sub.2 CH.sub.3 2-F-phenyl 2-(methylsulfonyl)phenyl                     1342 SO.sub.2 CH.sub.3 2-F-phenyl 4-morpholino                                 1343 SO.sub.2 CH.sub.3 2-F-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                  1344 SO.sub.2 CH.sub.3 2-F-phenyl 4-morpholinoc                               arbonyl                                                1345 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(aminosulfonyl)phenyl                  1346 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(methylaminosulfonyl)phenyl                                     1347 SO.sub.2 CH.sub.3 2,5-diF-phenyl 1-pyrroli                               dinocarbonyl                                           1348 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(methylsulfonyl)phenyl                 1349 SO.sub.2 CH.sub.3 2,5-diF-phenyl 4-morpholino                             1350 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phen                               yl                                                     1351 SO.sub.2 CH.sub.3 2,5-diF-phenyl 4-morpholinocarbonyl                     1352 SO.sub.2 CH.sub.3 phenyl 2-(N-pyrrolidinyl-methyl)phenyl                  1353 SO.sub.2 CH.sub.3 phenyl 2-(N-piperidinyl-methyl)phenyl                   1354 SO.sub.2 CH.sub.3 phenyl 2-(N-morpholino-methyl)phenyl                    1355 SO.sub.2 CH.sub.3 phenyl 2-(N,N'-methylmorpholinium-                         methyl)phenyl                                                               1356 SO.sub.2 CH.sub.3 phenyl 2-(N-pyridinium-methyl)phenyl                    1357 SO.sub.2 CH.sub.3 phenyl 2-(N-4-(N,N'-dimethylamino)-                        pyridinium-methyl)phenyl                                                    1358 SO.sub.2 CH.sub.3 phenyl 2-(N-azatanyl-methyl)phenyl                      1359 SO.sub.2 CH.sub.3 phenyl 2-(N-azetidinyl-methyl)phenyl                    1360 SO.sub.2 CH.sub.3 phenyl 2-(N-piperazinyl-methyl)phenyl                   1361 SO.sub.2 CH.sub.3 phenyl 2-(N,N'-BOC-piperazinyl-                            methyl)phenyl                                                               1362 SO.sub.2 CH.sub.3 phenyl 2-(N-imidazolyl-methyl)phenyl                    1363 SO.sub.2 CH.sub.3 phenyl 2-(N-methoxy-N-methylamino-                         methyl)phenyl                                                               1364 SO.sub.2 CH.sub.3 phenyl 2-(N-pyridonyl-methyl)phenyl                     1365 SO.sub.2 CH.sub.3 phenyl 2-(N-(N',N'-dimethylhydrazinyl-                     methyl)phenyl                                                               1366 SO.sub.2 CH.sub.3 phenyl 2-(amidinyl)phenyl                               1367 SO.sub.2 CH.sub.3 phenyl 2-(N-guanidinyl)phenyl                           1368 SO.sub.2 CH.sub.3 phenyl 2-(imidazolyl)phenyl                             1369 SO.sub.2 CH.sub.3 phenyl 2-(imidazolidinyl)phenyl                         1370 SO.sub.2 CH.sub.3 phenyl 2-(2-imidazolidinyl-                                sulfonyl)phenyl                                                             1371 SO.sub.2 CH.sub.3 phenyl 2-(2-pyrrolidinyl)phenyl                         1372 SO.sub.2 CH.sub.3 phenyl 2-(2-piperidinyl)phenyl                          1373 SO.sub.2 CH.sub.3 phenyl 2-(amidinyl-methyl)phenyl                        1374 SO.sub.2 CH.sub.3 phenyl 2-(2-imidazolidinyl-                                methyl)phenyl                                                               1375 SO.sub.2 CH.sub.3 phenyl 2-(N-(2-aminoimidazolyl)-                           methyl)phenyl                                                               1376 SO.sub.2 CH.sub.3 phenyl 2-dimethylaminoimidazol-1-yl                     1377 SO.sub.2 CH.sub.3 phenyl 2-(3-aminophenyl)                                1378 SO.sub.2 CH.sub.3 phenyl 2-(3-pyrrolidinylcarbonyl)                       1379 SO.sub.2 CH.sub.3 phenyl 2-glycinoyl                                      1380 SO.sub.2 CH.sub.3 phenyl 2-(imidazol-1-ylacetyl)                          1381 SO.sub.2 CH.sub.3 2-pyridyl 2-(N-pyrrolidinyl-methyl)phenyl                                        1382 SO.sub.2 CH.sub.3 2-pyridyl 2-(N-piperidin                               yl-methyl)phenyl                                       1383 SO.sub.2 CH.sub.3 2-pyridyl 2-(N-morpholino-methyl)phenyl                 1384 SO.sub.2 CH.sub.3 2-pyridyl 2-(N,N'-methylmorpholinium-                      methyl)phenyl                                                               1385 SO.sub.2 CH.sub.3 2-pyridyl 2-(N-pyridinium-methyl)phenyl                 1386 SO.sub.2 CH.sub.3 2-pyridyl 2-(N-4-(N,N'-dimethylamino)-                     pyridinium-methyl)phenyl                                                    1387 SO.sub.2 CH.sub.3 2-pyridyl 2-(N-azatanyl-methyl)phenyl                   1388 SO.sub.2 CH.sub.3 2-pyridyl 2-(N-azetidinyl-methyl)phenyl                 1389 SO.sub.2 CH.sub.3 2-pyridyl 2-(N-piperazinyl-methyl)phenyl                                         1390 SO.sub.2 CH.sub.3 2-pyridyl 2-(N,N'-BOC-pi                               perazinyl-                                                methyl)phenyl                                                               1391 SO.sub.2 CH.sub.3 2-pyridyl 2-(N-imidazolyl-methyl)phenyl                 1392 SO.sub.2 CH.sub.3 2-pyridyl 2-(N-methoxy-N-methylamino-                      methyl)phenyl                                                               1393 SO.sub.2 CH.sub.3 2-pyridyl 2-(N-pyridonyl-methyl)phenyl                  1394 SO.sub.2 CH.sub.3 2-pyridyl 2-(N-(N',N'-dimethylhydrazinyl-                                           methyl)phenyl                                      1395 SO.sub.2 CH.sub.3 2-pyridyl 2-(amidinyl)phenyl                            1396 SO.sub.2 CH.sub.3 2-pyridyl 2-(N-guanidinyl)phenyl                        1397 SO.sub.2 CH.sub.3 2-pyridyl 2-(imidazolyl)phenyl                          1398 SO.sub.2 CH.sub.3 2-pyridyl 2-(imidazolidinyl)phenyl                      1399 SO.sub.2 CH.sub.3 2-pyridyl 2-(2-imidazolidinyl-                             sulfonyl)phenyl                                                             1400 SO.sub.2 CH.sub.3 2-pyridyl 2-(2-pyrrolidinyl)phenyl                      1401 SO.sub.2 CH.sub.3 2-pyridyl 2-(2-piperidinyl)phenyl                       1402 SO.sub.2 CH.sub.3 2-pyridyl 2-(amidinyl-methyl)phenyl                     1403 SO.sub.2 CH.sub.3 2-pyridyl 2-(2-imidazolidinyl-                             methyl)phenyl                                                               1404 SO.sub.2 CH.sub.3 2-pyridyl 2-(N-(2-aminoimidazolyl)-                        methyl)phenyl                                                               1405 SO.sub.2 CH.sub.3 2-pyridyl 2-dimethylaminoimidazol-1-yl                  1406 SO.sub.2 CH.sub.3 2-pyridyl 2-(3-aminophenyl)                             1407 SO.sub.2 CH.sub.3 2-pyridyl 2-(3-pyrrolidinylcarbonyl)                    1408 SO.sub.2 CH.sub.3 2-pyridyl 2-glycinoyl                                   1409 SO.sub.2 CH.sub.3 2-pyridyl 2-(imidazol-1-ylacetyl)                       1410 SO.sub.2 CH.sub.3 3-pyridyl 2-(N-pyrrolidinyl-methyl)phenyl                                        1411 SO.sub.2 CH.sub.3 3-pyridyl 2-(N-piperidin                               yl-methyl)phenyl                                       1412 SO.sub.2 CH.sub.3 3-pyridyl 2-(N-morpholino-methyl)phenyl                 1413 SO.sub.2 CH.sub.3 3-pyridyl 2-(N,N'-methylmorpholinium-                      methyl)phenyl                                                               1414 SO.sub.2 CH.sub.3 3-pyridyl 2-(N-pyridinium-methyl)phenyl                 1415 SO.sub.2 CH.sub.3 3-pyridyl 2-(N-4-(N,N'-dimethylamino)-                     pyridinium-methyl)phenyl                                                    1416 SO.sub.2 CH.sub.3 3-pyridyl 2-(N-azatanyl-methyl)phenyl                   1417 SO.sub.2 CH.sub.3 3-pyridyl 2-(N-azetidinyl-methyl)phenyl                 1418 SO.sub.2 CH.sub.3 3-pyridyl 2-(N-piperazinyl-methyl)phenyl                                         1419 SO.sub.2 CH.sub.3 3-pyridyl 2-(N,N'-BOC-pi                               perazinyl-                                                methyl)phenyl                                                               1420 SO.sub.2 CH.sub.3 3-pyridyl 2-(N-imidazolyl-methyl)phenyl                 1421 SO.sub.2 CH.sub.3 3-pyridyl 2-(N-methoxy-N-methylamino-                      methyl)phenyl                                                               1422 SO.sub.2 CH.sub.3 3-pyridyl 2-(N-pyridonyl-methyl)phenyl                  1423 SO.sub.2 CH.sub.3 3-pyridyl 2-(N-(N',N'-dimethylhydrazinyl-                                           methyl)phenyl                                      1424 SO.sub.2 CH.sub.3 3-pyridyl 2-(amidinyl)phenyl                            1425 SO.sub.2 CH.sub.3 3-pyridyl 2-(N-guanidinyl)phenyl                        1426 SO.sub.2 CH.sub.3 3-pyridyl 2-(imidazolyl)phenyl                          1427 SO.sub.2 CH.sub.3 3-pyridyl 2-(imidazolidinyl)phenyl                      1428 SO.sub.2 CH.sub.3 3-pyridyl 2-(2-imidazolidinyl-                             sulfonyl)phenyl                                                             1429 SO.sub.2 CH.sub.3 3-pyridyl 2-(2-pyrrolidinyl)phenyl                      1430 SO.sub.2 CH.sub.3 3-pyridyl 2-(2-piperidinyl)phenyl                       1431 SO.sub.2 CH.sub.3 3-pyridyl 2-(amidinyl-methyl)phenyl                     1432 SO.sub.2 CH.sub.3 3-pyridyl 2-(2-imidazolidinyl-                             methyl)phenyl                                                               1433 SO.sub.2 CH.sub.3 3-pyridyl 2-(N-(2-aminoimidazolyl)-                        methyl)phenyl                                                               1434 SO.sub.2 CH.sub.3 3-pyridyl 2-dimethylaminoimidazol-1-yl                  1435 SO.sub.2 CH.sub.3 3-pyridyl 2-(3-aminophenyl)                             1436 SO.sub.2 CH.sub.3 3-pyridyl 2-(3-pyrrolidinylcarbonyl)                    1437 SO.sub.2 CH.sub.3 3-pyridyl 2-glycinoyl                                   1438 SO.sub.2 CH.sub.3 3-pyridyl 2-(imidazol-1-ylacetyl)                       1439 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-pyrrolidinyl-methyl)phenyl                                      1440 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-piperid                               inyl-methyl)phenyl                                     1441 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-morpholino-methyl)phenyl                                        1442 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(N,N'-meth                               ylmorpholinium-                                           methyl)phenyl                                                               1443 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-pyridinium-methyl)phenyl                                        1444 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-4-(N,N'                               -dimethylamino)-                                          pyridinium-methyl)phenyl                                                    1445 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-azatanyl-methyl)phenyl                 1446 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-azetidinyl-methyl)phenyl                                        1447 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-piperaz                               inyl-methyl)phenyl                                     1448 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(N,N'-BOC-piperazinyl-                       methyl)phenyl                                                               1449 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-imidazolyl-methyl)phenyl                                        1450 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-methoxy                               -N-methylamino-                                           methyl)phenyl                                                               1451 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-pyridonyl-methyl)phenyl                                         1452 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-(N',N'-                               dimethylhydrazinyl-                                       methyl)phenyl                                                               1453 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(amidinyl)phenyl                          1454 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-guanidinyl)phenyl                      1455 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(imidazolyl)phenyl                        1456 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(imidazolidinyl)phenyl                    1457 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(2-imidazolidinyl-                           sulfonyl)phenyl                                                             1458 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(2-pyrrolidinyl)phenyl                    1459 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(2-piperidinyl)phenyl                     1460 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(amidinyl-methyl)phenyl                   1461 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(2-imidazolidinyl-                           methyl)phenyl                                                               1462 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-(2-aminoimidazolyl)-                      methyl)phenyl                                                               1463 SO.sub.2 CH.sub.3 2-pyrimidyl 2-dimethylaminoimidazol-1-yl                                         1464 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(3-aminoph                               enyl)                                                  1465 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(3-pyrrolidinylcarbonyl)                  1466 SO.sub.2 CH.sub.3 2-pyrimidyl 2-glycinoyl                                 1467 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(imidazol-1-ylacetyl)                     1468 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-pyrrolidinyl-methyl)phenyl                                      1469 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-piperid                               inyl-methyl)phenyl                                     1470 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-morpholino-methyl)phenyl                                        1471 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N,N'-meth                               ylmorpholinium-                                           methyl)phenyl                                                               1472 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-pyridinium-methyl)phenyl                                        1473 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-4-(N,N'                               -dimethylamino)-                                          pyridinium-methyl)phenyl                                                    1474 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-azatanyl-methyl)phenyl                 1475 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-azetidinyl-methyl)phenyl                                        1476 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-piperaz                               inyl-methyl)phenyl                                     1477 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N,N'-BOC-piperazinyl-                       methyl)phenyl                                                               1478 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-imidazolyl-methyl)phenyl                                        1479 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-methoxy                               -N-methylamino-                                           methyl)phenyl                                                               1480 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-pyridonyl-methyl)phenyl                                         1481 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-(N',N'-                               dimethylhydrazinyl-                                       methyl)phenyl                                                               1482 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(amidinyl)phenyl                          1483 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-guanidinyl)phenyl                      1484 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(imidazolyl)phenyl                        1485 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(imidazolidinyl)phenyl                    1486 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(2-imidazolidinyl-                           sulfonyl)phenyl                                                             1487 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(2-pyrrolidinyl)phenyl                    1488 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(2-piperidinyl)phenyl                     1489 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(amidinyl-methyl)phenyl                   1490 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(2-imidazolidinyl-                           methyl)phenyl                                                               1491 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-(2-aminoimidazolyl)-                      methyl)phenyl                                                               1492 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-dimethylaminoimidazol-1-yl                                         1493 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(3-aminoph                               enyl)                                                  1494 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(3-pyrrolidinylcarbonyl)                  1495 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-glycinoyl                                 1496 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(imidazol-1-ylacetyl)                     1497 SO.sub.2 CH.sub.3 2-F-phenyl 2-(N-pyrrolidinyl-methyl)phenyl                                       1498 SO.sub.2 CH.sub.3 2-F-phenyl 2-(N-piperidi                               nyl-methyl)phenyl                                      1499 SO.sub.2 CH.sub.3 2-F-phenyl 2-(N-morpholino-methyl)phenyl                                         1500 SO.sub.2 CH.sub.3 2-F-phenyl 2-(N,N'-methy                               lmorpholinium-                                            methyl)phenyl                                                               1501 SO.sub.2 CH.sub.3 2-F-phenyl 2-(N-pyridinium-methyl)phenyl                                         1502 SO.sub.2 CH.sub.3 2-F-phenyl 2-(N-4-(N,N'-                               dimethylamino)-                                           pyridinium-methyl)phenyl                                                    1503 SO.sub.2 CH.sub.3 2-F-phenyl 2-(N-azatanyl-methyl)phenyl                  1504 SO.sub.2 CH.sub.3 2-F-phenyl 2-(N-azetidinyl-methyl)phenyl                                         1505 SO.sub.2 CH.sub.3 2-F-phenyl 2-(N-piperazi                               nyl-methyl)phenyl                                      1506 SO.sub.2 CH.sub.3 2-F-phenyl 2-(N,N'-BOC-piperazinyl-                        methyl)phenyl                                                               1507 SO.sub.2 CH.sub.3 2-F-phenyl 2-(N-imidazolyl-methyl)phenyl                                         1508 SO.sub.2 CH.sub.3 2-F-phenyl 2-(N-methoxy-                               N-methylamino-                                            methyl)phenyl                                                               1509 SO.sub.2 CH.sub.3 2-F-phenyl 2-(N-pyridonyl-methyl)phenyl                 1510 SO.sub.2 CH.sub.3 2-F-phenyl 2-(N-(N',N'-dimethylhydrazinyl-                                          methyl)phenyl                                      1511 SO.sub.2 CH.sub.3 2-F-phenyl 2-(amidinyl)phenyl                           1512 SO.sub.2 CH.sub.3 2-F-phenyl 2-(N-guanidinyl)phenyl                       1513 SO.sub.2 CH.sub.3 2-F-phenyl 2-(imidazolyl)phenyl                         1514 SO.sub.2 CH.sub.3 2-F-phenyl 2-(imidazolidinyl)phenyl                     1515 SO.sub.2 CH.sub.3 2-F-phenyl 2-(2-imidazolidinyl-                            sulfonyl)phenyl                                                             1516 SO.sub.2 CH.sub.3 2-F-phenyl 2-(2-pyrrolidinyl)phenyl                     1517 SO.sub.2 CH.sub.3 2-F-phenyl 2-(2-piperidinyl)phenyl                      1518 SO.sub.2 CH.sub.3 2-F-phenyl 2-(amidinyl-methyl)phenyl                    1519 SO.sub.2 CH.sub.3 2-F-phenyl 2-(2-imidazolidinyl-                            methyl)phenyl                                                               1520 SO.sub.2 CH.sub.3 2-F-phenyl 2-(N-(2-aminoimidazolyl)-                       methyl)phenyl                                                               1521 SO.sub.2 CH.sub.3 2-F-phenyl 2-dimethylaminoimidazol-1-yl                 1522 SO.sub.2 CH.sub.3 2-F-phenyl 2-(3-aminophenyl)                            1523 SO.sub.2 CH.sub.3 2-F-phenyl 2-(3-pyrrolidinylcarbonyl)                   1524 SO.sub.2 CH.sub.3 2-F-phenyl 2-glycinoyl                                  1525 SO.sub.2 CH.sub.3 2-F-phenyl 2-(imidazol-1-ylacetyl)                      1526 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N-pyrrolidinyl-methyl)phenyl                                   1527 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N-pipe                               ridinyl-methyl)phenyl                                  1528 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N-morpholino-methyl)phenyl                                     1529 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N,N'-m                               ethylmorpholinium-                                        methyl)phenyl                                                               1530 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N-pyridinium-methyl)phenyl                                     1531 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N-4-(N                               ,N'-dimethylamino)-                                       pyridinium-methyl)phenyl                                                    1532 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N-azatanyl-methyl)phenyl                                       1533 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N-azet                               idinyl-methyl)phenyl                                   1534 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N-piperazinyl-methyl)phenyl                                    1535 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N,N'-B                               OC-piperazinyl-                                           methyl)phenyl                                                               1536 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N-imidazolyl-methyl)phenyl                                     1537 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N-meth                               oxy-N-methylamino-                                        methyl)phenyl                                                               1538 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N-pyridonyl-methyl)phenyl                                      1539 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N-(N',                               N'-dimethylhydrazinyl-                                    methyl)phenyl                                                               1540 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(amidinyl)phenyl                       1541 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N-guanidinyl)phenyl                   1542 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(imidazolyl)phenyl                     1543 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(imidazolidinyl)phenyl                 1544 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(2-imidazolidinyl-                        sulfonyl)phenyl                                                             1545 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(2-pyrrolidinyl)phenyl                 1546 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(2-piperidinyl)phenyl                  1547 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(amidinyl-methyl)phenyl                                         1548 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(2-imid                               azolidinyl-                                               methyl)phenyl                                                               1549 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N-(2-aminoimidazolyl)-                                            methyl)phenyl                                      1550 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-dimethylaminoimidazol-1-yl                                      1551 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(3-amin                               ophenyl)                                               1552 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(3-pyrrolidinylcarbonyl)                                        1553 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-glycino                               yl                                                     1554 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(imidazol-1-ylacetyl)                  1555 NHSO.sub.2 CH.sub.3 phenyl 2-(aminosulfonyl)phenyl                        1556 NHSO.sub.2 CH.sub.3 phenyl 2-(methylaminosulfonyl)phenyl                  1557 NHSO.sub.2 CH.sub.3 phenyl 1-pyrrolidinocarbonyl                          1558 NHSO.sub.2 CH.sub.3 phenyl 2-(methylsulfonyl)phenyl                       1559 NHSO.sub.2 CH.sub.3 phenyl 4-morpholino                                   1560 NHSO.sub.2 CH.sub.3 phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                    1561 NHSO.sub.2 CH.sub.3 phenyl 4-morpholinocar                               bonyl                                                  1562 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(aminosulfonyl)phenyl                     1563 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(methylaminosulfonyl)phenyl                                        1564 NHSO.sub.2 CH.sub.3 2-pyridyl 1-pyrrolidin                               ocarbonyl                                              1565 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(methylsulfonyl)phenyl                    1566 NHSO.sub.2 CH.sub.3 2-pyridyl 4-morpholino                                1567 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl        1568 NHSO.sub.2 CH.sub.3 2-pyridyl 4-morpholinocarbonyl                        1569 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(aminosulfonyl)phenyl                     1570 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(methylaminosulfonyl)phenyl                                        1571 NHSO.sub.2 CH.sub.3 3-pyridyl 1-pyrrolidin                               ocarbonyl                                              1572 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(methylsulfonyl)phenyl                    1573 NHSO.sub.2 CH.sub.3 3-pyridyl 4-morpholino                                1574 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl        1575 NHSO.sub.2 CH.sub.3 3-pyridyl 4-morpholinocarbonyl                        1576 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(aminosulfonyl)phenyl                   1577 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(methylaminosulfonyl)phenyl                                      1578 NHSO.sub.2 CH.sub.3 2-pyrimidyl 1-pyrrolid                               inocarbonyl                                            1579 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(methylsulfonyl)phenyl                  1580 NHSO.sub.2 CH.sub.3 2-pyrimidyl 4-morpholino                              1581 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)pheny                               l                                                      1582 NHSO.sub.2 CH.sub.3 2-pyrimidyl 4-morpholinocarbonyl                      1583 NHSO.sub.2 CH.sub.3 5-pyrimidyl 2-(aminosulfonyl)phenyl                   1584 NHSO.sub.2 CH.sub.3 5-pyrimidyl 2-(methylaminosulfonyl)phenyl                                      1585 NHSO.sub.2 CH.sub.3 5-pyrimidyl 1-pyrrolid                               inocarbonyl                                            1586 NHSO.sub.2 CH.sub.3 5-pyrimidyl 2-(methylsulfonyl)phenyl                  1587 NHSO.sub.2 CH.sub.3 5-pyrimidyl 4-morpholino                              1588 NHSO.sub.2 CH.sub.3 5-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)pheny                               l                                                      1589 NHSO.sub.2 CH.sub.3 5-pyrimidyl 4-morpholinocarbonyl                      1590 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(aminosulfonyl)phenyl                   1591 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(methylaminosulfonyl)phenyl                                      1592 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 1-pyrrolid                               inocarbonyl                                            1593 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(methylsulfonyl)phenyl                  1594 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 4-morpholino                              1595 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)pheny                               l                                                      1596 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 4-morpholinocarbonyl                      1597 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(aminosulfonyl)phenyl                    1598 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(methylaminosulfonyl)phenyl                                       1599 NHSO.sub.2 CH.sub.3 2-F-phenyl 1-pyrrolidi                               nocarbonyl                                             1600 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(methylsulfonyl)phenyl                   1601 NHSO.sub.2 CH.sub.3 2-F-phenyl 4-morpholino                               1602 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl       1603 NHSO.sub.2 CH.sub.3 2-F-phenyl 4-morpholinocarbonyl                       1604 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(aminosulfonyl)phenyl                                         1605 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl                                       2-(methylaminosulfonyl)phenyl                          1606 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 1-pyrrolidinocarbonyl                  1607 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(methylsulfonyl)phenyl                                        1608 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl                                       4-morpholino                                           1609 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)ph                               enyl                                                   1610 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 4-morpholinocarbonyl                   1611 NHSO.sub.2 CH.sub.3 phenyl 2-(N-pyrrolidinyl-methyl)phenyl                                         1612 NHSO.sub.2 CH.sub.3 phenyl 2-(N-piperidiny                               l-methyl)phenyl                                        1613 NHSO.sub.2 CH.sub.3 phenyl 2-(N-morpholino-methyl)phenyl                  1614 NHSO.sub.2 CH.sub.3 phenyl 2-(N,N'-methylmorpholinium-                       methyl)phenyl                                                               1615 NHSO.sub.2 CH.sub.3 phenyl 2-(N-pyridinium-methyl)phenyl                  1616 NHSO.sub.2 CH.sub.3 phenyl 2-(N-4-(N,N'-dimethylamino)-                      pyridinium-methyl)phenyl                                                    1617 NHSO.sub.2 CH.sub.3 phenyl 2-(N-azatanyl-methyl)phenyl                    1618 NHSO.sub.2 CH.sub.3 phenyl 2-(N-azetidinyl-methyl)phenyl                  1619 NHSO.sub.2 CH.sub.3 phenyl 2-(N-piperazinyl-methyl)phenyl                 1620 NHSO.sub.2 CH.sub.3 phenyl 2-(N,N'-BOC-piperazinyl-                          methyl)phenyl                                                               1621 NHSO.sub.2 CH.sub.3 phenyl 2-(N-imidazolyl-methyl)phenyl                  1622 NHSO.sub.2 CH.sub.3 phenyl 2-(N-methoxy-N-methylamino-                       methyl)phenyl                                                               1623 NHSO.sub.2 CH.sub.3 phenyl 2-(N-pyridonyl-methyl)phenyl                   1624 NHSO.sub.2 CH.sub.3 phenyl 2-(N-(N',N'-dimethylhydrazinyl-                                            methyl)phenyl                                      1625 NHSO.sub.2 CH.sub.3 phenyl 2-(amidinyl)phenyl                             1626 NHSO.sub.2 CH.sub.3 phenyl 2-(N-guanidinyl)phenyl                         1627 NHSO.sub.2 CH.sub.3 phenyl 2-(imidazolyl)phenyl                           1628 NHSO.sub.2 CH.sub.3 phenyl 2-(imidazolidinyl)phenyl                       1629 NHSO.sub.2 CH.sub.3 phenyl 2-(2-imidazolidinyl-                              sulfonyl)phenyl                                                             1630 NHSO.sub.2 CH.sub.3 phenyl 2-(2-pyrrolidinyl)phenyl                       1631 NHSO.sub.2 CH.sub.3 phenyl 2-(2-piperidinyl)phenyl                        1632 NHSO.sub.2 CH.sub.3 phenyl 2-(amidinyl-methyl)phenyl                      1633 NHSO.sub.2 CH.sub.3 phenyl 2-(2-imidazolidinyl-                              methyl)phenyl                                                               1634 NHSO.sub.2 CH.sub.3 phenyl 2-(N-(2-aminoimidazolyl)-                         methyl)phenyl                                                               1635 NHSO.sub.2 CH.sub.3 phenyl 2-dimethylaminoimidazol-1-yl                   1636 NHSO.sub.2 CH.sub.3 phenyl 2-(3-aminophenyl)                              1637 NHSO.sub.2 CH.sub.3 phenyl 2-(3-pyrrolidinylcarbonyl)                     1638 NHSO.sub.2 CH.sub.3 phenyl 2-glycinoyl                                    1639 NHSO.sub.2 CH.sub.3 phenyl 2-(imidazol-1-ylacetyl)                        1640 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(N-pyrrolidinyl-methyl)phenyl                                      1641 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(N-piperid                               inyl-methyl)phenyl                                     1642 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(N-morpholino-methyl)phenyl                                        1643 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(N,N'-meth                               ylmorpholinium-                                           methyl)phenyl                                                               1644 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(N-pyridinium-methyl)phenyl                                        1645 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(N-4-(N,N'                               -dimethylamino)-                                          pyridinium-methyl)phenyl                                                    1646 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(N-azatanyl-methyl)phenyl                 1647 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(N-azetidinyl-methyl)phenyl                                        1648 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(N-piperaz                               inyl-methyl)phenyl                                     1649 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(N,N'-BOC-piperazinyl-                       methyl)phenyl                                                               1650 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(N-imidazolyl-methyl)phenyl                                        1651 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(N-methoxy                               -N-methylamino-                                           methyl)phenyl                                                               1652 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(N-pyridonyl-methyl)phenyl                                         1653 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(N-(N',N'-                               dimethylhydrazinyl-                                       methyl)phenyl                                                             1654 NHSO.sub.2 CH.sub.3                                                                      2-pyridyl  2-(amidinyl)phenyl                                     1655 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(N-guanidinyl)phenyl                      1656 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(imidazolyl)phenyl                        1657 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(imidazolidinyl)phenyl                    1658 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(2-imidazolidinyl-                           sulfonyl)phenyl                                                             1659 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(2-pyrrolidinyl)phenyl                    1660 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(2-piperidinyl)phenyl                     1661 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(amidinyl-methyl)phenyl                   1662 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(2-imidazolidinyl-                           methyl)phenyl                                                               1663 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(N-(2-aminoimidazolyl)-                      methyl)phenyl                                                               1664 NHSO.sub.2 CH.sub.3 2-pyridyl 2-dimethylaminoimidazol-1-yl                                         1665 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(3-aminoph                               enyl)                                                  1666 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(3-pyrrolidinylcarbonyl)                  1667 NHSO.sub.2 CH.sub.3 2-pyridyl 2-glycinoyl                                 1668 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(imidazol-1-ylacetyl)                     1669 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(N-pyrrolidinyl-methyl)phenyl                                      1670 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(N-piperid                               inyl-methyl)phenyl                                     1671 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(N-morpholino-methyl)phenyl                                        1672 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(N,N'-meth                               ylmorpholinium-                                           methyl)phenyl                                                               1673 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(N-pyridiniuin-methyl)phenyl                                       1674 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(N-4-(N,N'                               -dimethylamino)-                                          pyridinium-methyl)phenyl                                                    1675 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(N-azatanyl-methyl)phenyl                 1676 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(N-azetidinyl-methyl)phenyl                                        1677 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(N-piperaz                               inyl-methyl)phenyl                                     1678 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(N,N'-BOC-piperazinyl-                       methyl)phenyl                                                               1679 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(N-imidazolyl-methyl)phenyl                                        1680 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(N-methoxy                               -N-methylamino-                                           methyl)phenyl                                                               1681 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(N-pyridonyl-methyl)phenyl                                         1682 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(N-(N',N'-                               dimethylhydrazinyl-                                       methyl)phenyl                                                               1683 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(amidinyl)phenyl                          1684 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(N-guanidinyl)phenyl                      1685 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(imidazolyl)phenyl                        1686 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(imidazolidinyl)phenyl                    1687 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(2-imidazolidinyl-                           sulfonyl)phenyl                                                             1688 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(2-pyrrolidinyl)phenyl                    1689 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(2-piperidinyl)phenyl                     1690 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(amidinyl-methyl)phenyl                   1691 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(2-imidazolidinyl-                           methyl)phenyl                                                               1692 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(N-(2-aminoimidazolyl)-                      methyl)phenyl                                                               1693 NHSO.sub.2 CH.sub.3 3-pyridyl 2-dimethylaminoimidazol-1-yl                                         1694 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(3-aminoph                               enyl)                                                  1695 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(3-pyrrolidinylcarbonyl)                  1696 NHSO.sub.2 CH.sub.3 3-pyridyl 2-glycinoyl                                 1697 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(imidazol-1-ylacetyl)                     1698 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-pyrrolidinyl-methyl)phenyl                                    1699 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-piper                               idinyl-methyl)phenyl                                   1700 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-morpholino-methyl)phenyl                                      1701 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(N,N'-me                               thylmorpholinium-                                         methyl)phenyl                                                               1702 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-pyridinium-methyl)phenyl                                      1703 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-4-(N,                               N'-dimethylamino)-                                        pyridinium-methyl)phenyl                                                    1704 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-azatanyl-methyl)phenyl                                        1705 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-azeti                               dinyl-methyl)phenyl                                    1706 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-piperazinyl-methyl)phenyl                                     1707 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(N,N'-BO                               C-piperazinyl-                                            methyl)phenyl                                                               1708 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-imidazolyl-methyl)phenyl                                      1709 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-metho                               xy-N-methylamino-                                         methyl)phenyl                                                               1710 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-pyridonyl-methyl)phenyl                                       1711 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-(N',N                               '-dimethylhydrazinyl-                                     methyl)phenyl                                                               1712 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(amidinyl)phenyl                        1713 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-guanidinyl)phenyl                    1714 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(imidazolyl)phenyl                      1715 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(imidazolidinyl)phenyl                  1716 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(2-imidazolidinyl-                         sulfonyl)phenyl                                                             1717 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(2-pyrrolidinyl)phenyl                  1718 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(2-piperidinyl)phenyl                   1719 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(amidinyl-methyl)phenyl                 1720 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(2-imidazolidinyl-                         methyl)phenyl                                                               1721 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(N-(2-aminoimidazolyl)-                    methyl)phenyl                                                               1722 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-dimethylaminoimidazol-1-yl                                       1723 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(3-amino                               phenyl)                                                1724 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(3-pyrrolidinylcarbonyl)                                         1725 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-glycinoy                               l                                                      1726 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(imidazol-1-ylacetyl)                   1727 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-pyrrolidinyl-methyl)phenyl                                    1728 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-piper                               idinyl-methyl)phenyl                                   1729 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-morpholino-methyl)phenyl                                      1730 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N,N'-me                               thylmorpholinium-                                         methyl)phenyl                                                               1731 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-pyridinium-methyl)phenyl                                      1732 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-4-(N,                               N'-dimethylamino)-                                        pyridinium-methyl)phenyl                                                    1733 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-azatanyl-methyl)phenyl                                        1734 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-azeti                               dinyl-methyl)phenyl                                    1735 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-piperazinyl-methyl)phenyl                                     1736 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N,N'-BO                               C-piperazinyl-                                            methyl)phenyl                                                               1737 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-imidazolyl-methyl)phenyl                                      1738 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-metho                               xy-N-methylamino-                                         methyl)phenyl                                                               1739 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-pyridonyl-methyl)phenyl                                       1740 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-(N',N                               '-dimethylhydrazinyl-                                     methyl)phenyl                                                               1741 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(amidinyl)phenyl                        1742 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-guanidinyl)phenyl                    1743 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(imidazolyl)phenyl                      1744 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(imidazolidinyl)phenyl                  1745 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(2-imidazolidinyl-                         sulfonyl)phenyl                                                             1746 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(2-pyrrolidinyl)phenyl                  1747 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(2-piperidinyl)phenyl                   1748 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(amidinyl-methyl)phenyl                 1749 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(2-imidazolidinyl-                         methyl)phenyl                                                               1750 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(N-(2-aminoimidazolyl)-                    methyl)phenyl                                                               1751 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-dimethylaminoimidazol-1-yl                                       1752 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(3-amino                               phenyl)                                                1753 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(3-pyrrolidinylcarbonyl)                                         1754 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-glycinoy                               l                                                      1755 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(imidazol-1-ylacetyl)                   1756 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(N-pyrrolidinyl-methyl)phenyl                                     1757 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(N-piperi                               dinyl-methyl)phenyl                                    1758 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(N-morpholino-methyl)phenyl                                       1759 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(N,N'-met                               hylmorpholinium-                                          methyl)phenyl                                                               1760 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(N-pyridinium-methyl)phenyl                                       1761 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(N-4-(N,N                               '-dimethylamino)-                                         pyridinium-methyl)phenyl                                                    1762 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(N-azatanyl-methyl)phenyl                                         1763 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(N-azetid                               inyl-methyl)phenyl                                     1764 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(N-piperazinyl-methyl)phenyl                                      1765 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(N,N'-BOC                               -piperazinyl-                                             methyl)phenyl                                                               1766 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(N-imidazolyl-methyl)phenyl                                       1767 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(N-methox                               y-N-methylamino-                                          methyl)phenyl                                                               1768 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(N-pyridonyl-methyl)phenyl                                        1769 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(N-(N',N'                               -dimethylhydrazinyl-                                      methyl)phenyl                                                               1770 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(amidinyl)phenyl                         1771 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(N-guanidinyl)phenyl                     1772 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(imidazolyl)phenyl                       1773 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(imidazolidinyl)phenyl                   1774 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(2-imidazolidinyl-                          sulfonyl)phenyl                                                             1775 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(2-pyrrolidinyl)phenyl                   1776 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(2-piperidinyl)phenyl                    1777 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(amidinyl-methyl)phenyl                  1778 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(2-imidazolidinyl-                          methyl)phenyl                                                               1779 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(N-(2-aminoimidazolyl)-                     methyl)phenyl                                                               1780 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-dimethylaminoimidazol-1-yl                                        1781 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(3-aminop                               henyl)                                                 1782 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(3-pyrrolidinylcarbonyl)                 1783 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-glycinoyl                                1784 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(imidazol-1-ylacetyl)                    1785 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N-pyrrolidinyl-methyl)phenyl        1786 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N-piperidinyl-methyl)phenyl                                  1787 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl                                       2-(N-morpholino-methyl)phenyl                          1788 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N,N'-methylmorpholinium-                                        methyl)phenyl                                      1789 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N-pyridinium-methyl)phenyl                                   1790 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl                                       2-(N-4-(N,N'-dimethylamino)-                              pyridinium-methyl)phenyl                                                    1791 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N-azatanyl-methyl)phenyl                                     1792 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl                                       2-(N-azetidinyl-methyl)phenyl                          1793 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N-piperazinyl-methyl)phenyl                                  1794 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl                                       2-(N,N'-BOC-piperazinyl-                                  methyl)phenyl                                                               1795 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N-imidazolyl-methyl)phenyl                                   1796 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl                                       2-(N-methoxy-N-methylamino-                               methyl)phenyl                                                               1797 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N-pyridonyl-methyl)phenyl                                    1798 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl                                       2-(N-(N',N'-dimethylhydrazinyl-                           methyl)phenyl                                                               1799 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(amidinyl)phenyl                     1800 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N-guanidinyl)phenyl                 1801 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(imidazolyl)phenyl                   1802 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(imidazolidinyl)phenyl                                        1803 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl                                       2-(2-imidazolidinyl-                                      sulfonyl)phenyl                                                             1804 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(2-pyrrolidinyl)phenyl                                        1805 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl                                       2-(2-piperidinyl)phenyl                                1806 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(amidinyl-methyl)phenyl                                       1807 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl                                       2-(2-imidazolidinyl-                                      methyl)phenyl                                                               1808 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(N-(2-aminoimidazolyl)-                                          methyl)phenyl                                      1809 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 2-dimethylaminoimidazol-1-yl                                    1810 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl                                       2-(3-aminophenyl)                                      1811 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(3-pyrrolidinylcarbonyl)                                      1812 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl                                       2-glycinoyl                                            1813 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(imidazol-1-ylacetyl)              ______________________________________                                    

                                      TABLE 3                                      __________________________________________________________________________      ##STR74##                                                                     __________________________________________________________________________                                                 #STR75##                                                                       #STR76##                                                                      ##STR77##                           __________________________________________________________________________     a.sub.1                                                                           R = F, D = NH.sub.2                                                                              b.sub.1                                                                           R = F, D = NH.sub.2                                                                              c.sub.1                                                                           R = F, D = NH.sub.2                 a.sub.2 R = H, D = NH.sub.2 b.sub.2 R = H, D = NH.sub.2 c.sub.2 R = H,                                                    D = NH.sub.2                        a.sub.3 R = F, D = CH.sub.2 NH.sub.2 b.sub.3 R = F, D = CH.sub.2                                                          NH.sub.2 c.sub.3 R = F, D =                                                    CH.sub.2 NH.sub.2                   a.sub.4 R = H, D = CH.sub.2 NH.sub.2 b.sub.4 R = H, D = CH.sub.2                                                          NH.sub.2 c.sub.4 R = H, D =                                                    CH.sub.2 NH.sub.2                   a.sub.5 R = F, D = C(═NH)NH.sub.2 b.sub.5 R = F, D = C(═NH)NH.su                                                  b.2 c.sub.5 R = F, D =                                                         C(═NH)NH.sub.2                  a.sub.6 R = H, D = C(═NH)NH.sub.2 b.sub.6 R = H, D = C(═NH)NH.su                                                  b.2 c.sub.6 R = H, D =                                                         C(═NH)NH.sub.2                  a.sub.7 R = F, D = C(O)NH.sub.2 b.sub.7 R = F, D = C(O)NH.sub.2 c.sub.7                                                   R = F, D = C(O)NH.sub.2                                                         a.sub.8 R = H, D = C(O)NH.su                                                  b.2 b.sub.8 R = H, D =                                                         C(O)NH.sub.2 c.sub.8 R = H,                                                    D = C(O)NH.sub.2                  __________________________________________________________________________                                                 #STR78##                                                                       #STR79##                                                                      ##STR80##                           __________________________________________________________________________     d.sub.1                                                                           R = F, D = NH.sub.2                                                                              e.sub.1                                                                           R = F, D = NH.sub.2                                                                              f.sub.1                                                                           R = F, D = NH.sub.2                 d.sub.2 R = H, D = NH.sub.2 e.sub.2 R = H, D = NH.sub.2 f.sub.2 R = H,                                                    D = NH.sub.2                        d.sub.3 R = F, D = CH.sub.2 NH.sub.2 e.sub.3 R = F, D = CH.sub.2                                                          NH.sub.2 f.sub.3 R = F, D =                                                    CH.sub.2 NH.sub.2                   d.sub.4 R = H, D = CH.sub.2 NH.sub.2 e.sub.4 R = H, D = CH.sub.2                                                          NH.sub.2 f.sub.4 R = H, D =                                                    CH.sub.2 NH.sub.2                   d.sub.5 R = F, D = C(═NH)NH.sub.2 e.sub.5 R = F, D = C(═NH)NH.su                                                  b.2 f.sub.5 R = F, D =                                                         C(═NH)NH.sub.2                  d.sub.6 R = H, D = C(═NH)NH.sub.2 e.sub.6 R = H, D = C(═NH)NH.su                                                  b.2 f.sub.6 R = H, D =                                                         C(═NH)NH.sub.2                  d.sub.7 R = F, D = C(O)NH.sub.2 e.sub.7 R = F, D = C(O)NH.sub.2 f.sub.7                                                   R = F, D = C(O)NH.sub.2                                                         d.sub.8 R = H, D = C(O)NH.su                                                  b.2 e.sub.8 R = H, D =                                                         C(O)NH.sub.2 f.sub.8 R = H,                                                    D = C(O)NH.sub.2                  __________________________________________________________________________                                                 #STR81##                                                                       #STR82##                                                                      ##STR83##                           __________________________________________________________________________     g.sub.1                                                                           R = F, D = NH.sub.2                                                                              h.sub.1                                                                           R = F, D = NH.sub.2                                                                              i.sub.1                                                                           R = F, D = NH.sub.2                 g.sub.2 R = H, D = NH.sub.2 h.sub.2 R = H, D = NH.sub.2 i.sub.2 R = H,                                                    D = NH.sub.2                        g.sub.3 R = F, D = CH.sub.2 NH.sub.2 h.sub.3 R = F, D = CH.sub.2                                                          NH.sub.2 i.sub.3 R = F, D =                                                    CH.sub.2 NH.sub.2                   g.sub.4 R = H, D = CH.sub.2 NH.sub.2 h.sub.4 R = H, D = CH.sub.2                                                          NH.sub.2 i.sub.4 R = H, D =                                                    CH.sub.2 NH.sub.2                   g.sub.5 R = F, D = C(═NH)NH.sub.2 h.sub.5 R = F, D = C(═NH)NH.su                                                  b.2 i.sub.5 R = F, D =                                                         C(═NH)NH.sub.2                  g.sub.6 R = H, D = C(═NH)NH.sub.2 h.sub.6 R = H, D = C(═NH)NH.su                                                  b.2 i.sub.6 R = H, D =                                                         C(═NH)NH.sub.2                  g.sub.7 R = F, D = C(O)NH.sub.2 h.sub.7 R = F, D = C(O)NH.sub.2 i.sub.7                                                   R = F, D = C(O)NH.sub.2                                                         g.sub.8 R = H, D = C(O)NH.su                                                  b.2 h.sub.8 R = H, D =                                                         C(O)NH.sub.2 i.sub.8 R = H,                                                    D = C(O)NH.sub.2                  __________________________________________________________________________                                                 #STR84##                                                                       #STR85##                                                                      ##STR86##                           __________________________________________________________________________     j.sub.1                                                                           R = F, D = NH.sub.2                                                                              k.sub.1                                                                           R = F, D = NH.sub.2                                                                              l.sub.1                                                                           R = F, D = NH.sub.2                 j.sub.2 R = H, D = NH.sub.2 k.sub.2 R = H, D = NH.sub.2 l.sub.2 R = H,                                                    D = NH.sub.2                        j.sub.3 R = F, D = CH.sub.2 NH.sub.2 k.sub.3 R = F, D = CH.sub.2                                                          NH.sub.2 l.sub.3 R = F, D =                                                    CH.sub.2 NH.sub.2                   j.sub.4 R = H, D = CH.sub.2 NH.sub.2 k.sub.4 R = H, D = CH.sub.2                                                          NH.sub.2 l.sub.4 R = H, D =                                                    CH.sub.2 NH.sub.2                   j.sub.5 R = F, D = C(═NH)NH.sub.2 k.sub.5 R = F, D = C(═NH)NH.su                                                  b.2 l.sub.5 R = F, D =                                                         C(═NH)NH.sub.2                  j.sub.6 R = H, D = C(═NH)NH.sub.2 k.sub.6 R = H, D = C(═NH)NH.su                                                  b.2 l.sub.6 R = H, D =                                                         C(═NH)NH.sub.2                  j.sub.7 R = F, D = C(O)NH.sub.2 k.sub.7 R = F, D = C(O)NH.sub.2 l.sub.7                                                   R = F, D = C(O)NH.sub.2                                                         j.sub.8 R = H, D = C(O)NH.su                                                  b.2 k.sub.8 R = H, D =                                                         C(O)NH.sub.2 l.sub.8 R = H,                                                    D = C(O)NH.sub.2                  __________________________________________________________________________                                                 #STR87##                                                                       #STR88##                                                                      ##STR89##                           __________________________________________________________________________     m.sub.1                                                                           R = F, D = NH.sub.2                                                                              n.sub.1                                                                           R = F, D = NH.sub.2                                                                              o.sub.1                                                                           R = F, D = NH.sub.2                 m.sub.2 R = H, D = NH.sub.2 n.sub.2 R = H, D = NH.sub.2 o.sub.2 R = H,                                                    D = NH.sub.2                        m.sub.3 R = F, D = CH.sub.2 NH.sub.2 n.sub.3 R = F, D = CH.sub.2                                                          NH.sub.2 o.sub.3 R = F, D =                                                    CH.sub.2 NH.sub.2                   m.sub.4 R = H, D = CH.sub.2 NH.sub.2 n.sub.4 R = H, D = CH.sub.2                                                          NH.sub.2 o.sub.4 R = H, D =                                                    CH.sub.2 NH.sub.2                   m.sub.5 R = F, D = C(═NH)NH.sub.2 n.sub.5 R = F, D = C(═NH)NH.su                                                  b.2 o.sub.5 R = F, D =                                                         C(═NH)NH.sub.2                  m.sub.6 R = H, D = C(═NH)NH.sub.2 n.sub.6 R = H, D = C(═NH)NH.su                                                  b.2 o.sub.6 R = H, D =                                                         C(═NH)NH.sub.2                  m.sub.7 R = F, D = C(O)NH.sub.2 n.sub.7 R = F, D = C(O)NH.sub.2 o.sub.7                                                   R = F, D = C(O)NH.sub.2                                                         m.sub.8 R = H, D = C(O)NH.su                                                  b.2 n.sub.8 R = H, D =                                                         C(O)NH.sub.2 o.sub.8 R = H,                                                    D = C(O)NH.sub.2                  __________________________________________________________________________                                                 #STR90##                                                                       #STR91##                                                                      ##STR92##                           __________________________________________________________________________     p.sub.1                                                                           R = F, D = NH.sub.2                                                                              q.sub.1                                                                           R = F, D = NH.sub.2                                                                              r.sub.1                                                                           R = F, D = NH.sub.2                 p.sub.2 R = Cl, D = NH.sub.2 q.sub.2 R = Cl, D = NH.sub.2 r.sub.2 R =                                                     Cl, D = NH.sub.2                    p.sub.3 R = OMe, D = NH.sub.2 q.sub.3 R = OMe, D = NH.sub.2 r.sub.3 R =                                                   OMe, D = NH.sub.2                   p.sub.4 R = F, D = CH.sub.2 NH.sub.2 q.sub.4 R = F, D = CH.sub.2                                                          NH.sub.2 r.sub.4 R = F, D =                                                    CH.sub.2 NH.sub.2                   p.sub.5 R = Cl, D = CH.sub.2 NH.sub.2 q.sub.5 R = Cl, D = CH.sub.2                                                        NH.sub.2 r.sub.5 R = Cl, D =                                                   CH.sub.2 NH.sub.2                   p.sub.6 R = OMe, D = CH.sub.2 NH.sub.2 q.sub.6 R = OMe, D = CH.sub.2                                                      NH.sub.2 r.sub.6 R = OMe, D                                                    = CH.sub.2 NH.sub.2                 p.sub.7 R = F, D = C(═NH)NH.sub.2 q.sub.7 R = F, D = C(═NH)NH.su                                                  b.2 r.sub.7 R = F, D =                                                         C(═NH)NH.sub.2                  p.sub.8 R = Cl, D = C(═NH)NH.sub.2 q.sub.8 R = Cl, D = C(═NH)NH.                                                  sub.2 r.sub.8 R = Cl, D =                                                      C(═NH)NH.sub.2                  p.sub.9 R = OMe, D = C(═NH)NH.sub.2 q.sub.9 R = OMe, D = C(═NH)N                                                  H.sub.2 r.sub.9 R = OMe, D =                                                   C(═NH)NH.sub.2                  p.sub.10 R = F, D = C(O)NH.sub.2 q.sub.10 R = F, D = C(O)NH.sub.2                                                         r.sub.10 R = F, D = C(O)NH.su                                                  b.2                                 p.sub.11 R = Cl, D = C(O)NH.sub.2 q.sub.11 R = Cl, D = C(O)NH.sub.2                                                       r.sub.11 R = Cl, D =                                                           C(O)NH.sub.2                        p.sub.12 R = OMe, D = C(O)NH.sub.2 q.sub.12 R = OMe, D = C(O)NH.sub.2                                                     r.sub.12 R = OMe, D =                                                          C(O)NH.sub.2                      __________________________________________________________________________                                                 #STR93##                                                                       #STR94##                                                                      ##STR95##                           __________________________________________________________________________     s.sub.1                                                                           R = F, D = NH.sub.2                                                                              t.sub.1                                                                           R = F, D = NH.sub.2                                                                              u.sub.1                                                                           R = F, D = NH.sub.2                 s.sub.2 R = Cl, D = NH.sub.2 t.sub.2 R = Cl, D = NH.sub.2 u.sub.2 R =                                                     Cl, D = NH.sub.2                    s.sub.3 R = OMe, D = NH.sub.2 t.sub.3 R = OMe, D = NH.sub.2 u.sub.3 R =                                                   OMe, D = NH.sub.2                   s.sub.4 R = F, D = CH.sub.2 NH.sub.2 t.sub.4 R = F, D = CH.sub.2                                                          NH.sub.2 u.sub.4 R = F, D =                                                    CH.sub.2 NH.sub.2                   s.sub.5 R = Cl, D = CH.sub.2 NH.sub.2 t.sub.5 R = Cl, D = CH.sub.2                                                        NH.sub.2 u.sub.5 R = Cl, D =                                                   CH.sub.2 NH.sub.2                   s.sub.6 R = OMe, D = CH.sub.2 NH.sub.2 t.sub.6 R = OMe, D = CH.sub.2                                                      NH.sub.2 u.sub.6 R = OMe, D                                                    = CH.sub.2 NH.sub.2                 s.sub.7 R = F, D = C(═NH)NH.sub.2 t.sub.7 R = F, D = C(═NH)NH.su                                                  b.2 u.sub.7 R = F, D =                                                         C(═NH)NH.sub.2                  s.sub.8 R = Cl, D = C(═NH)NH.sub.2 t.sub.8 R = Cl, D = C(═NH)NH.                                                  sub.2 u.sub.8 R = Cl, D =                                                      C(═NH)NH.sub.2                  s.sub.9 R = OMe, D = C(═NH)NH.sub.2 t.sub.9 R = OMe, D = C(═NH)N                                                  H.sub.2 u.sub.9 R = OMe, D =                                                   C(═NH)NH.sub.2                  s.sub.10 R = F, D = C(O)NH.sub.2 t.sub.10 R = F, D = C(O)NH.sub.2                                                         u.sub.10 R = F, D = C(O)NH.su                                                  b.2                                 s.sub.11 R = Cl, D = C(O)NH.sub.2 t.sub.11 R = Cl, D = C(O)NH.sub.2                                                       u.sub.11 R = Cl, D =                                                           C(O)NH.sub.2                        s.sub.12 R = OMe, D = C(O)NH.sub.2 t.sub.12 R = OMe, D = C(O)NH.sub.2                                                     u.sub.12 R = OMe, D =                                                          C(O)NH.sub.2                      __________________________________________________________________________                                                 #STR96##                                                                       #STR97##                                                                      ##STR98##                           __________________________________________________________________________     v.sub.1                                                                           R = F, D = NH.sub.2                                                                              w.sub.1                                                                           R = F, D = NH.sub.2                                                                              x.sub.1                                                                           R = F, D = NH.sub.2                 v.sub.2 R = Cl, D = NH.sub.2 w.sub.2 R = Cl, D = NH.sub.2 x.sub.2 R =                                                     Cl, D = NH.sub.2                    v.sub.3 R = OMe, D = NH.sub.2 w.sub.3 R = OMe, D = NH.sub.2 x.sub.3 R =                                                   OMe, D = NH.sub.2                   v.sub.4 R = F, D = CH.sub.2 NH.sub.2 w.sub.4 R = F, D = CH.sub.2                                                          NH.sub.2 x.sub.4 R = F, D =                                                    CH.sub.2 NH.sub.2                   v.sub.5 R = Cl, D = CH.sub.2 NH.sub.2 w.sub.5 R = Cl, D = CH.sub.2                                                        NH.sub.2 x.sub.5 R = Cl, D =                                                   CH.sub.2 NH.sub.2                   v.sub.6 R = OMe, D = CH.sub.2 NH.sub.2 w.sub.6 R = OMe, D = CH.sub.2                                                      NH.sub.2 x.sub.6 R = OMe, D                                                    = CH.sub.2 NH.sub.2                 v.sub.7 R = F, D = C(═NH)NH.sub.2 w.sub.7 R = F, D = C(═NH)NH.su                                                  b.2 x.sub.7 R = F, D =                                                         C(═NH)NH.sub.2                  v.sub.8 R = Cl, D = C(═NH)NH.sub.2 w.sub.8 R = Cl, D = C(═NH)NH.                                                  sub.2 x.sub.8 R = Cl, D =                                                      C(═NH)NH.sub.2                  v.sub.9 R = OMe, D = C(═NH)NH.sub.2 w.sub.9 R = OMe, D = C(═NH)N                                                  H.sub.2 x.sub.9 R = OMe, D =                                                   C(═NH)NH.sub.2                  v.sub.10 R = F, D = C(O)NH.sub.2 w.sub.10 R = F, D = C(O)NH.sub.2                                                         x.sub.10 R = F, D = C(O)NH.su                                                  b.2                                 v.sub.11 R = Cl, D = C(O)NH.sub.2 w.sub.11 R = Cl, D = C(O)NH.sub.2                                                       x.sub.11 R = Cl, D =                                                           C(O)NH.sub.2                        v.sub.12 R = OMe, D = C(O)NH.sub.2 w.sub.12 R = OMe, D = C(O)NH.sub.2                                                     x.sub.12 R = OMe, D =                                                          C(O)NH.sub.2                      __________________________________________________________________________                                                 #STR99##                                                                       #STR100##                                                                     ##STR101##                          __________________________________________________________________________     y.sub.1                                                                           R = F, D = NH.sub.2                                                                              z.sub.1                                                                           R = F, D = NH.sub.2                                                                              aa.sub.1                                                                          R = F, D = NH.sub.2                 y.sub.2 R = Cl, D = NH.sub.2 z.sub.2 R = Cl, D = NH.sub.2 aa.sub.2 R =                                                    Cl, D = NH.sub.2                    y.sub.3 R = OMe, D = NH.sub.2 z.sub.3 R = OMe, D = NH.sub.2 aa.sub.3 R                                                    = OMe, D = NH.sub.2                 y.sub.4 R = F, D = CH.sub.2 NH.sub.2 z.sub.4 R = F, D = CH.sub.2                                                          NH.sub.2 aa.sub.4 R = F, D =                                                   CH.sub.2 NH.sub.2                   y.sub.5 R = Cl, D = CH.sub.2 NH.sub.2 z.sub.5 R = Cl, D = CH.sub.2                                                        NH.sub.2 aa.sub.5 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 y.sub.6 R = OMe, D = CH.sub.2 NH.sub.2 z.sub.6 R = OMe, D = CH.sub.2                                                      NH.sub.2 aa.sub.6 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 y.sub.7 R = F, D = C(═NH)NH.sub.2 z.sub.7 R = F, D = C(═NH)NH.su                                                  b.2 aa.sub.7 R = F, D =                                                        C(═NH)NH.sub.2                  y.sub.8 R = Cl, D = C(═NH)NH.sub.2 z.sub.8 R = Cl, D = C(═NH)NH.                                                  sub.2 aa.sub.8 R = Cl, D =                                                     C(═NH)NH.sub.2                  y.sub.9 R = OMe, D = C(═NH)NH.sub.2 z.sub.9 R = OMe, D = C(═NH)N                                                  H.sub.2 aa.sub.9 R = OMe, D                                                    = C(═NH)NH.sub.2                                                            y.sub.10 R = F, D =                                                           C(O)NH.sub.2 z.sub.10 R = F,                                                   D = C(O)NH.sub.2 aa.sub.10 R                                                   = F, D = C(O)NH.sub.2                                                           y.sub.11 R = Cl, D =                                                          C(O)NH.sub.2 z.sub.11 R =                                                      Cl, D = C(O)NH.sub.2                                                           aa.sub.11 R = Cl, D =                                                          C(O)NH.sub.2                        y.sub.12 R = OMe, D = C(O)NH.sub.2 z.sub.12 R = OMe, D = C(O)NH.sub.2                                                     aa.sub.12 R = OMe, D =                                                         C(O)NH.sub.2                      __________________________________________________________________________                                                 #STR102##                                                                      #STR103##                                                                     ##STR104##                          __________________________________________________________________________     bb.sub.1                                                                          R = F, D = NH.sub.2                                                                              cc.sub.1                                                                          R = F, D = NH.sub.2                                                                              dd.sub.1                                                                          R = F, D = NH.sub.2                 bb.sub.2 R = Cl, D = NH.sub.2 cc.sub.2 R = Cl, D = NH.sub.2 dd.sub.2 R                                                    = Cl, D = NH.sub.2                  bb.sub.3 R = OMe, D = NH.sub.2 cc.sub.3 R = OMe, D = NH.sub.2 dd.sub.3                                                    R = OMe, D = NH.sub.2                                                           bb.sub.4 R = F, D =                                                           CH.sub.2 NH.sub.2 cc.sub.4 R                                                   = F, D = CH.sub.2 NH.sub.2                                                     dd.sub.4 R = F, D = CH.sub.2                                                   NH.sub.2                            bb.sub.5 R = Cl, D = CH.sub.2 NH.sub.2 cc.sub.5 R = Cl, D = CH.sub.2                                                      NH.sub.2 dd.sub.5 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 bb.sub.6 R = OMe, D = CH.sub.2 NH.sub.2 cc.sub.6 R = OMe, D = CH.sub.2                                                    NH.sub.2 dd.sub.6 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 bb.sub.7 R = F, D = C(═NH)NH.sub.2 cc.sub.7 R = F, D = C(═NH)NH.                                                  sub.2 dd.sub.7 R = F, D =                                                      C(═NH)NH.sub.2                  bb.sub.8 R = Cl, D = C(═NH)NH.sub.2 cc.sub.8 R = Cl, D = C(═NH)N                                                  H.sub.2 dd.sub.8 R = Cl, D =                                                   C(═NH)NH.sub.2                  bb.sub.9 R = OMe, D = C(═NH)NH.sub.2 cc.sub.9 R = OMe, D = C(═NH                                                  )NH.sub.2 dd.sub.9 R = OMe,                                                    D = C(═NH)NH.sub.2                                                          bb.sub.10 R = F, D =                                                          C(O)NH.sub.2 cc.sub.10 R =                                                     F, D = C(O)NH.sub.2 dd.sub.10                                                   R = F, D = C(O)NH.sub.2                                                        bb.sub.11 R = Cl, D =                                                         C(O)NH.sub.2 cc.sub.11 R =                                                     Cl, D = C(O)NH.sub.2                                                           dd.sub.11 R = Cl, D =                                                          C(O)NH.sub.2                        bb.sub.12 R = OMe, D = C(O)NH.sub.2 cc.sub.12 R = OMe, D = C(O)NH.sub.2                                                   dd.sub.12 R = OMe, D =                                                         C(O)NH.sub.2                      __________________________________________________________________________                                                 #STR105##                                                                      #STR106##                                                                     ##STR107##                          __________________________________________________________________________     ee.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     ff.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     gg.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2        ee.sub.2 R = Cl, D = CH.sub.2 NH.sub.2 ff.sub.2 R = Cl, D = CH.sub.2                                                      NH.sub.2 gg.sub.2 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 ee.sub.3 R = OMe, D = CH.sub.2 NH.sub.2 ff.sub.3 R = OMe, D = CH.sub.2                                                    NH.sub.2 gg.sub.3 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 ee.sub.4 R = CH.sub.2 NH.sub.2, ff.sub.4 R = CH.sub.2 NH.sub.2,                                                           gg.sub.4 R = CH.sub.2                                                          NH.sub.2,                            D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2         __________________________________________________________________________                                                 #STR108##                                                                      #STR109##                                                                     ##STR110##                          __________________________________________________________________________     hh.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     ii.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     jj.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2        hh.sub.2 R = Cl, D = CH.sub.2 NH.sub.2 ii.sub.2 R = Cl, D = CH.sub.2                                                      NH.sub.2 jj.sub.2 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 hh.sub.3 R = OMe, D = CH.sub.2 NH.sub.2 ii.sub.3 R = OMe, D = CH.sub.2                                                    NH.sub.2 jj.sub.3 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 hh.sub.4 R = CH.sub.2 NH.sub.2, ii.sub.4 R = CH.sub.2 NH.sub.2,                                                           jj.sub.4 R = CH.sub.2                                                          NH.sub.2,                            D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2         __________________________________________________________________________                                                 #STR111##                                                                      #STR112##                                                                     ##STR113##                          __________________________________________________________________________     kk.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     ll.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     mm.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2        kk.sub.2 R = Cl, D = CH.sub.2 NH.sub.2 ll.sub.2 R = Cl, D = CH.sub.2                                                      NH.sub.2 mm.sub.2 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 kk.sub.3 R = OMe, D = CH.sub.2 NH.sub.2 ll.sub.3 R = OMe, D = CH.sub.2                                                    NH.sub.2 mm.sub.3 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 kk.sub.4 R = CH.sub.2 NH.sub.2, ll.sub.4 R = CH.sub.2 NH.sub.2,                                                           mm.sub.4 R = CH.sub.2                                                          NH.sub.2,                            D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2         __________________________________________________________________________                                                 #STR114##                                                                      #STR115##                                                                     ##STR116##                          __________________________________________________________________________     nn.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     oo.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     pp.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2        nn.sub.2 R = Cl, D = CH.sub.2 NH.sub.2 oo.sub.2 R = Cl, D = CH.sub.2                                                      NH.sub.2 pp.sub.2 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 nn.sub.3 R = OMe, D = CH.sub.2 NH.sub.2 oo.sub.3 R = OMe, D = CH.sub.2                                                    NH.sub.2 pp.sub.3 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 nn.sub.4 R = CH.sub.2 NH.sub.2, oo.sub.4 R = CH.sub.2 NH.sub.2,                                                           pp.sub.4 R = CH.sub.2                                                          NH.sub.2,                            D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2         __________________________________________________________________________                                                 #STR117##                                                                      #STR118##                                                                     ##STR119##                          __________________________________________________________________________     qq.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     rr.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     ss.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2        qq.sub.2 R = Cl, D = CH.sub.2 NH.sub.2 rr.sub.2 R = Cl, D = CH.sub.2                                                      NH.sub.2 ss.sub.2 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 qq.sub.3 R = OMe, D = CH.sub.2 NH.sub.2 rr.sub.3 R = OMe, D = CH.sub.2                                                    NH.sub.2 ss.sub.3 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 qq.sub.4 R = CH.sub.2 NH.sub.2, rr.sub.4 R = CH.sub.2 NH.sub.2,                                                           ss.sub.4 R = CH.sub.2                                                          NH.sub.2,                            D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2         __________________________________________________________________________

    ______________________________________                                         Ex#  R.sup.1b  A           B                                                   ______________________________________                                         1    H         phenyl      2-((Me).sub.2 N-methyl)phenyl                         2 H phenyl 2-((Me)NH-methyl)phenyl                                             3 H phenyl 2-(H.sub.2 N-methyl)phenyl                                          4 H phenyl 2-HOCH.sub.2 -phenyl                                                5 H 2-F-phenyl 2-((Me).sub.2 N-methyl)phenyl                                   6 H 2-F-phenyl 2-((Me)NH-methyl)phenyl                                         7 H 2-F-phenyl 2-(H.sub.2 N-methyl)phenyl                                      8 H 2-F-phenyl 2-HOCH.sub.2 -phenyl                                            9 H phenyl 2-methylimidazol-1-yl                                               10 H phenyl 2-ethylimidazol-1-yl                                               11 H phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                               12 H phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                                 13 H phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                                14 H 2-F-phenyl 2-methylimidazol-1-yl                                          15 H 2-F-phenyl 2-ethylimidazol-1-yl                                           16 H 2-F-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                           17 H 2-F-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                             18 H 2-F-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                            19 H 2-Cl-phenyl 2-methylimidazol-1-yl                                         20 H 2-Cl-phenyl 2-ethylimidazol-1-yl                                          21 H 2-Cl-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                          22 H 2-Cl-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                            23 H 2-Cl-phenyl 2-CH.sub.3 OCH.sub.2 -imidazo1-1-y1                           24 H 2-(Me).sub.2 N-phenyl 2-methylimidazol-1-yl                               25 H 2-(Me).sub.2 N-phenyl 2-ethylimidazol-1-yl                                26 H 2-(Me).sub.2 N-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                                          27 H 2-(Me).sub.2 N-phenyl 2-CH.sub.3                                         SO.sub.2 -imidazol-1-yl                               28 H 2-(Me).sub.2 N-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                 29 H phenyl N-methylimidazol-2-yl                                              30 H phenyl 4-methylimidazol-5-yl                                              31 H phenyl 5-CF.sub.3 -pyrazol-1-yl                                           32 H 2-F-phenyl N-methylimidazol-2-yl                                          33 H 2-F-phenyl 4-methylimidazol-5-yl                                          34 H 2-F-phenyl 5-CF.sub.3 -pyrazol-1-yl                                       35 H phenyl guanidino                                                          36 H phenyl 2-thiazolin-2-ylamine                                              37 H phenyl N-methyl-2-imidazolin-2-yl                                         38 H phenyl N-methyl-1,4,5,6-                                                     tetrahydropyrimid-2-yl                                                      39 H phenyl N-methylimidazol-2-ylthiol                                         40 H phenyl t-butoxycarbonylamine                                              41 H phenyl (N-pyrrolidino)formylimino                                         42 H phenyl (N-pyrrolidino)formyl-N-                                              (methanesulfamoyl)imino                                                     43 H 2-F-phenyl guanidino                                                      44 H 2-F-phenyl 2-thiazolin-2-ylamine                                          45 H 2-F-phenyl N-methyl-2-imidazolin-2-yl                                     46 H 2-F-phenyl N-methyl-1,4,5,6-                                                 tetrahydropyrimid-2-yl                                                      47 H 2-F-phenyl N-methylimidazol-2-ylthio                                      48 H 2-F-phenyl t-butoxycarbonylamine                                          49 H 2-F-phenyl (N-pyrrolidino)formylimino                                     50 H 2-F-phenyl (N-pyrrolidino)formyl-N-                                          (methanesulfamoyl)imino                                                     51 H 2-CH.sub.3 O-phenyl (N-pyrrolidino)formylimino                            52 H 2-CH.sub.3 O-phenyl (N-pyrrolidino)formyl-N-                                 (methanesulfamoyl)imino                                                     53 --CN phenyl 2-((Me).sub.2 N-methyl)phenyl                                   54 --CN phenyl 2-((Me)NH-methyl)phenyl                                         55 --CN phenyl 2-(H.sub.2 N-methyl)phenyl                                      56 --CN phenyl 2-HOCH.sub.2 -phenyl                                            57 --CN 2-F-phenyl 2-((Me).sub.2 N-methyl)phenyl                               58 --CN 2-F-phenyl 2-((Me)NH-methyl)phenyl                                     59 --CN 2-F-phenyl 2-(H.sub.2 N-methyl)phenyl                                  60 --CN 2-F-phenyl 2-HOCH.sub.2 -phenyl                                        61 --CN phenyl 2-methylimidazol-1-yl                                           62 --CN phenyl 2-ethylimidazol-1-yl                                            63 --CN phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                            64 --CN phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                              65 --CN phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                             66 --CN 2-F-phenyl 2-methylimidazol-1-yl                                       67 --CN 2-F-phenyl 2-ethylimidazol-1-yl                                        68 --CN 2-F-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                        69 --CN 2-F-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                          70 --CN 2-F-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                         71 --CN 2-Cl-phenyl 2-methylimidazol-1-yl                                      72 --CN 2-Cl-phenyl 2-ethylimidazol-1-yl                                       73 --CN 2-Cl-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                       74 --CN 2-Cl-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                         75 --CN 2-Cl-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                        76 --CN 2-(Me).sub.2 N-phenyl 2-methylimidazol-1-yl                            77 --CN 2-(Me).sub.2 N-phenyl 2-ethylimidazol-1-yl                             78 --CN 2-(Me).sub.2 N-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                                       79 --CN 2-(Me).sub.2 N-phenyl 2-CH.sub.3                                      SO.sub.2 -imidazol-1-yl                               80 --CN 2-(Me).sub.2 N-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                                        81 --CN phenyl N-methylimidazol-2-yl                 82 --CN phenyl 4-methylimidazol-5-yl                                           83 --CN phenyl 5-CF.sub.3 -pyrazol-1-yl                                        84 --CN 2-F-phenyl N-methylimidazol-2-yl                                       85 --CN 2-F-phenyl 4-methylimidazol-5-yl                                       86 --CN 2-F-phenyl 5-CF.sub.3 -pyrazol-1-yl                                    87 --CN phenyl guanidino                                                       88 --CN phenyl 2-thiazolin-2-ylamine                                           89 --CN phenyl N-methyl-2-imidazolin-2-yl                                      90 --CN phenyl N-methyl-1,4,5,6-                                                  tetrahydropyrimid-2-yl                                                      91 --CN phenyl N-methylimidazol-2-ylthiol                                      92 --CN phenyl t-butoxycarbonylamine                                           93 --CN phenyl (N-pyrrolidino)formylimino                                      94 --CN phenyl (N-pyrrolidino)formyl-N-                                           (methanesulfamoyl)imino                                                     95 --CN 2-F-phenyl guanidino                                                   96 --CN 2-F-phenyl 2-thiazolin-2-ylamine                                       97 --CN 2-F-phenyl N-methyl-2-imidazolin-2-yl                                  98 --CN 2-F-phenyl N-methyl-1,4,5,6-                                              tetrahydropyrimid-2-yl                                                      99 --CN 2-F-phenyl N-methylimidazol-2-ylthio                                   100 --CN 2-F-phenyl t-butoxycarbonylamine                                      101 --CN 2-F-phenyl (N-pyrrolidino)formylimino                                 102 --CN 2-F-phenyl (N-pyrrolidino)formyl-N-                                      (methanesulfamoyl)imino                                                     103 --CN 2-CH.sub.3 O-phenyl (N-pyrrolidino)formylimino                        104 --CN 2-CH.sub.3 O-phenyl (N-pyrrolidino)formyl-N-                             (methanesulfamoyl)imino                                                     105 CF.sub.3  phenyl 2-((Me).sub.2 N-methyl)phenyl                             106 CF.sub.3  phenyl 2-((Me)NH-methyl)phenyl                                   107 CF.sub.3  phenyl 2-(H.sub.2 N-methyl)phenyl                                108 CF.sub.3  phenyl 2-HOCH.sub.2 -phenyl                                      109 CF.sub.3  2-F-phenyl 2-((Me).sub.2 N-methyl)phenyl                         110 CF.sub.3  2-F-phenyl 2-((Me)NH-methyl)phenyl                               111 CF.sub.3  2-F-phenyl 2-(H.sub.2 N-methyl)phenyl                            112 CF.sub.3  2-F-phenyl 2-HOCH.sub.2 -phenyl                                  113 CF.sub.3  phenyl 2-methylimidazol-1-yl                                     114 CF.sub.3  phenyl 2-ethylimidazol-1-yl                                      115 CF.sub.3  phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                      116 CF.sub.3  phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                        117 CF.sub.3  phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                       118 CF.sub.3  2-F-phenyl 2-methylimidazol-1-yl                                 119 CF.sub.3  2-F-phenyl 2-ethylimidazol-1-yl                                  120 CF.sub.3  2-F-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                  121 CF.sub.3  2-F-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                    122 CF.sub.3  2-F-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                   123 CF.sub.3  2-Cl-phenyl 2-methylimidazol-1-yl                                124 CF.sub.3  2-Cl-phenyl 2-ethylimidazol-1-yl                                 125 CF.sub.3  2-Cl-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                 126 CF.sub.3  2-Cl-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                   127 CF.sub.3  2-Cl-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                  128 CF.sub.3  2-(Me).sub.2 N-phenyl 2-methylimidazol-1-yl                      129 CF.sub.3  2-(Me).sub.2 N-phenyl 2-ethylimidazol-1-yl                       130 CF.sub.3  2-(Me).sub.2 N-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl       131 CF.sub.3  2-(Me).sub.2 N-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                                   132 CF.sub.3  2-(Me).sub.2 N-phenyl 2-CH.sub.3                                 OCH.sub.2 -imidazol-1-yl                             133 CF.sub.3  phenyl N-methylimidazol-2-yl                                     134 CF.sub.3  phenyl 4-methylimidazol-5-yl                                     135 CF.sub.3  phenyl 5-CF.sub.3 -pyrazol-1-yl                                  136 CF.sub.3  2-F-phenyl N-methylimidazol-2-yl                                 137 CF.sub.3  2-F-phenyl 4-methylimidazol-5-yl                                 138 CF.sub.3  2-F-phenyl 5-CF.sub.3 -pyrazol-1-yl                              139 CF.sub.3  phenyl guanidino                                                 140 CF.sub.3  phenyl 2-thiazolin-2-ylamine                                     141 CF.sub.3  phenyl N-methyl-2-imidazolin-2-yl                                142 CF.sub.3  phenyl N-methyl-1,4,5,6-                                            tetrahydropyrimid-2-yl                                                      143 CF.sub.3  phenyl N-methylimidazol-2-ylthiol                                144 CF.sub.3  phenyl t-butoxycarbonylamine                                     145 CF.sub.3  phenyl (N-pyrrolidino)formylimino                                146 CF.sub.3  phenyl (N-pyrrolidino)formyl-N-                                     (methanesulfamoyl)imino                                                     147 CF.sub.3  2-F-phenyl guanidino                                             148 CF.sub.3  2-F-phenyl 2-thiazolin-2-ylamine                                 149 CF.sub.3  2-F-phenyl N-methyl-2-imidazolin-2-yl                            150 CF.sub.3  2-F-phenyl N-methyl-1,4,5,6-                                        tetrahydropyrimid-2-yl                                                      151 CF.sub.3  2-F-phenyl N-methylimidazol-2-ylthio                             152 CF.sub.3  2-F-phenyl t-butoxycarbonylamine                                 153 CF.sub.3  2-F-phenyl (N-pyrrolidino)formylimino                            154 CF.sub.3  2-F-phenyl (N-pyrrolidino)formyl-N-                                 (methanesulfamoyl)imino                                                     155 CF.sub.3  2-CH.sub.3 O-phenyl (N-pyrrolidino)formylimino                   156 CF.sub.3  2-CH.sub.3 O-phenyl (N-pyrrolidino)formyl-N-                        (methanesulfamoyl)imino                                                     157 CONH.sub.2 phenyl 2-((Me).sub.2 N-methyl)phenyl                            158 CONH.sub.2 phenyl 2-((Me)NH-methyl)phenyl                                  159 CONH.sub.2 phenyl 2-(H.sub.2 N-methyl)phenyl                               160 CONH.sub.2 phenyl 2-HOCH.sub.2 -phenyl                                     161 CONH.sub.2 2-F-phenyl 2-((Me).sub.2 N-methyl)phenyl                        162 CONH.sub.2 2-F-phenyl 2-((Me)NH-methyl)phenyl                              163 CONH.sub.2 2-F-phenyl 2-(H.sub.2 N-methyl)phenyl                           164 CONH.sub.2 2-F-phenyl 2-HOCH.sub.2 -phenyl                                 165 CONH.sub.2 phenyl 2-methylimidazol-1-yl                                    166 CONH.sub.2 phenyl 2-ethylimidazol-1-yl                                     167 CONH.sub.2 phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                     168 CONH.sub.2 phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                       169 CONH.sub.2 phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                      170 CONH.sub.2 2-F-phenyl 2-methylimidazol-1-yl                                171 CONH.sub.2 2-F-phenyl 2-ethylimidazol-1-yl                                 172 CONH.sub.2 2-F-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                 173 CONH.sub.2 2-F-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                   174 CONH.sub.2 2-F-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                  175 CONH.sub.2 2-Cl-phenyl 2-methylimidazol-1-yl                               176 CONH.sub.2 2-Cl-phenyl 2-ethylimidazol-1-yl                                177 CONH.sub.2 2-Cl-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                                          178 CONH.sub.2 2-Cl-phenyl 2-CH.sub.3                                         SO.sub.2 -imidazol-1-yl                               179 CONH.sub.2 2-Cl-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                 180 CONH.sub.2 2-(Me).sub.2 N-phenyl 2-methylimidazol-1-yl                     181 CONH.sub.2 2-(Me).sub.2 N-phenyl 2-ethylimidazol-1-yl                      182 CONH.sub.2 2-(Me).sub.2 N-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-y                                l                                                     183 CONH.sub.2 2-(Me).sub.2 N-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl        184 CONH.sub.2 2-(Me).sub.2 N-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl       185 CONH.sub.2 phenyl N-methylimidazol-2-yl                                    186 CONH.sub.2 phenyl 4-methylimidazol-5-yl                                    187 CONH.sub.2 phenyl 5-CF.sub.3 -pyrazol-1-yl                                 188 CONH.sub.2 2-F-phenyl N-methylimidazol-2-yl                                189 CONH.sub.2 2-F-phenyl 4-methylimidazol-5-yl                                190 CONH.sub.2 2-F-phenyl 5-CF.sub.3 -pyrazol-1-yl                             191 CONH.sub.2 phenyl guanidino                                                192 CONH.sub.2 phenyl 2-thiazolin-2-ylamine                                    193 CONH.sub.2 phenyl N-methyl-2-imidazolin-2-yl                               194 CONH.sub.2 phenyl N-methyl-1,4,5,6-                                           tetrahydropyrimid-2-yl                                                      195 CONH.sub.2 phenyl N-methylimidazol-2-ylthiol                               196 CONH.sub.2 phenyl t-butoxycarbonylamine                                    197 CONH.sub.2 phenyl (N-pyrrolidino)formylimino                               198 CONH.sub.2 phenyl (N-pyrrolidino)formyl-N-                                    (methanesulfamoyl)imino                                                     199 CONH.sub.2 2-F-phenyl guanidino                                            200 CONH.sub.2 2-F-phenyl 2-thiazolin-2-ylamine                                201 CONH.sub.2 2-F-phenyl N-methyl-2-imidazolin-2-yl                           202 CONH.sub.2 2-F-phenyl N-methyl-1,4,5,6-                                       tetrahydropyrimid-2-yl                                                      203 CONH.sub.2 2-F-phenyl N-methylimidazol-2-ylthio                            204 CONH.sub.2 2-F-phenyl t-butoxycarbonylamine                                205 CONH.sub.2 2-F-phenyl (N-pyrrolidino)formylimino                           206 CONH.sub.2 2-F-phenyl (N-pyrrolidino)formyl-N-                                (methanesulfamoyl)imino                                                     207 CONH.sub.2 2-CH.sub.3 O-phenyl (N-pyrrolidino)formylimino                  208 CONH.sub.2 2-CH.sub.3 O-phenyl (N-pyrrolidino)formyl-N-                       (methanesulfamoyl)imino                                                     209 SCH.sub.3 phenyl 2-((Me).sub.2 N-methyl)phenyl                             210 SCH.sub.3 phenyl 2-((Me)NH-methyl)phenyl                                   211 SCH.sub.3 phenyl 2-(H.sub.2 N-methyl)phenyl                                212 SCH.sub.3 phenyl 2-HOCH.sub.2 -phenyl                                      213 SCH.sub.3 2-F-phenyl 2-((Me).sub.2 N-methyl)phenyl                         214 SCH.sub.3 2-F-phenyl 2-((Me)NH-methyl)phenyl                               215 SCH.sub.3 2-F-phenyl 2-(H.sub.2 N-methyl)phenyl                            216 SCH.sub.3 2-F-phenyl 2-HOCH.sub.2 -phenyl                                  217 SCH.sub.3 phenyl 2-methylimidazol-1-yl                                     218 SCH.sub.3 phenyl 2-ethylimidazol-1-yl                                      219 SCH.sub.3 phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                      220 SCH.sub.3 phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                        221 SCH.sub.3 phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                       222 SCH.sub.3 2-F-phenyl 2-methylimidazol-1-yl                                 223 SCH.sub.3 2-F-phenyl 2-ethylimidazol-1-yl                                  224 SCH.sub.3 2-F-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                  225 SCH.sub.3 2-F-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                    226 SCH.sub.3 2-F-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                   227 SCH.sub.3 2-Cl-phenyl 2-methylimidazol-1-yl                                228 SCH.sub.3 2-Cl-phenyl 2-ethylimidazol-1-yl                                 229 SCH.sub.3 2-Cl-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                 230 SCH.sub.3 2-Cl-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                   231 SCH.sub.3 2-Cl-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                  232 SCH.sub.3 2-(Me).sub.2 N-phenyl 2-methylimidazol-1-yl                      233 SCH.sub.3 2-(Me).sub.2 N-phenyl 2-ethylimidazol-1-yl                       234 SCH.sub.3 2-(Me).sub.2 N-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl       235 SCH.sub.3 2-(Me).sub.2 N-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                                   236 SCH.sub.3 2-(Me).sub.2 N-phenyl 2-CH.sub.3                                 OCH.sub.2 -imidazol-1-yl                             237 SCH.sub.3 phenyl N-methylimidazol-2-yl                                     238 SCH.sub.3 phenyl 4-methylimidazol-5-yl                                     239 SCH.sub.3 phenyl 5-CF.sub.3 -pyrazol-1-yl                                  240 SCH.sub.3 2-F-phenyl N-methylimidazol-2-yl                                 241 SCH.sub.3 2-F-phenyl 4-methylimidazol-5-yl                                 242 SCH.sub.3 2-F-phenyl 5-CF.sub.3 -pyrazol-1-yl                              243 SCH.sub.3 phenyl guanidino                                                 244 SCH.sub.3 phenyl 2-thiazolin-2-ylamine                                     245 SCH.sub.3 phenyl N-methyl-2-imidazolin-2-yl                                246 SCH.sub.3 phenyl N-methyl-1,4,5,6-                                            tetrahydropyrimid-2-yl                                                      247 SCH.sub.3 phenyl N-methylimidazol-2-ylthiol                                248 SCH.sub.3 phenyl t-butoxycarbonylamine                                     249 SCH.sub.3 phenyl (N-pyrrolidino)formylimino                                250 SCH.sub.3 phenyl (N-pyrrolidino)formyl-N-                                     (methanesulfamoyl)imino                                                     251 SCH.sub.3 2-F-phenyl guanidino                                             252 SCH.sub.3 2-F-phenyl 2-thiazolin-2-ylamine                                 253 SCH.sub.3 2-F-phenyl N-methyl-2-imidazolin-2-yl                            254 SCH.sub.3 2-F-phenyl N-methyl-1,4,5,6-                                        tetrahydropyrimid-2-yl                                                      255 SCH.sub.3 2-F-phenyl N-methylimidazol-2-ylthio                             256 SCH.sub.3 2-F-phenyl t-butoxycarbonylamine                                 257 SCH.sub.3 2-F-phenyl (N-pyrrolidino)formylimino                            258 SCH.sub.3 2-F-phenyl (N-pyrrolidino)formyl-N-                                 (methanesulfamoyl)imino                                                     259 SCH.sub.3 2-CH.sub.3 O-phenyl (N-pyrrolidino)formylimino                   260 SCH.sub.3 2-CH.sub.3 O-phenyl (N-pyrrolidino)formyl-N-                        (methanesulfamoyl)imino                                                     261 SO.sub.2 CH.sub.3 phenyl 2-((Me).sub.2 N-methyl)phenyl                     262 SO.sub.2 CH.sub.3 phenyl 2-((Me)NH-methyl)phenyl                           263 SO.sub.2 CH.sub.3 phenyl 2-(H.sub.2 N-methyl)phenyl                        264 SO.sub.2 CH.sub.3 phenyl 2-HOCH.sub.2 -phenyl                              265 SO.sub.2 CH.sub.3 2-F-phenyl 2-((Me).sub.2 N-methyl)phenyl                 266 SO.sub.2 CH.sub.3 2-F-phenyl 2-((Me)NH-methyl)phenyl                       267 SO.sub.2 CH.sub.3 2-F-phenyl 2-(H.sub.2 N-methyl)phenyl                    268 SO.sub.2 CH.sub.3 2-F-phenyl 2-HOCH.sub.2 -phenyl                          269 SO.sub.2 CH.sub.3 phenyl 2-methylimidazol-1-yl                             270 SO.sub.2 CH.sub.3 phenyl 2-ethylimidazol-1-yl                              271 SO.sub.2 CH.sub.3 phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                                        272 SO.sub.2 CH.sub.3 phenyl 2-CH.sub.3                                       SO.sub.2 -imidazol-1-yl                               273 SO.sub.2 CH.sub.3 phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                                         274 SO.sub.2 CH.sub.3 2-F-phenyl 2-methylimida                                zol-1-yl                                              275 SO.sub.2 CH.sub.3 2-F-phenyl 2-ethylimidazol-1-yl                          276 SO.sub.2 CH.sub.3 2-F-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                                    277 SO.sub.2 CH.sub.3 2-F-phenyl 2-CH.sub.3                                   SO.sub.2 -imidazol-1-yl                               278 SO.sub.2 CH.sub.3 2-F-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                                     279 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-methylimid                                azol-1-yl                                             280 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-ethylimidazol-1-yl                         281 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                                   282 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-CH.sub.3                                  SO.sub.2 -imidazol-1-yl                               283 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                                    284 SO.sub.2 CH.sub.3 2-(Me).sub.2 N-phenyl                                   2-methylimidazol-1-yl                                 285 SO.sub.2 CH.sub.3 2-(Me).sub.2 N-phenyl 2-ethylimidazol-1-yl                                         286 SO.sub.2 CH.sub.3 2-(Me).sub.2 N-phenyl                                   2-((Me).sub.2 N-methyl)imidazol-1-yl                  287 SO.sub.2 CH.sub.3 2-(Me).sub.2 N-phenyl 2-CH.sub.3 SO.sub.2                                         -imidazol-1-yl                                        288 SO.sub.2 CH.sub.3 2-(Me).sub.2 N-phenyl 2-CH.sub.3 OCH.sub.2                                        -imidazol-1-yl                                        289 SO.sub.2 CH.sub.3 phenyl N-methylimidazol-2-yl                             290 SO.sub.2 CH.sub.3 phenyl 4-methylimidazol-5-yl                             291 SO.sub.2 CH.sub.3 phenyl 5-CF.sub.3 -pyrazol-1-yl                          292 SO.sub.2 CH.sub.3 2-F-phenyl N-methylimidazol-2-yl                         293 SO.sub.2 CH.sub.3 2-F-phenyl 4-methylimidazol-5-yl                         294 SO.sub.2 CH.sub.3 2-F-phenyl 5-CF.sub.3 -pyrazol-1-yl                      295 SO.sub.2 CH.sub.3 phenyl guanidino                                         296 SO.sub.2 CH.sub.3 phenyl 2-thiazolin-2-ylamine                             297 SO.sub.2 CH.sub.3 phenyl N-methyl-2-imidazolin-2-yl                        298 SO.sub.2 CH.sub.3 phenyl N-methyl-1,4,5,6-                                    tetrahydropyrimid-2-yl                                                      299 SO.sub.2 CH.sub.3 phenyl N-methylimidazol-2-ylthiol                        300 SO.sub.2 CH.sub.3 phenyl t-butoxycarbonylamine                             301 SO.sub.2 CH.sub.3 phenyl (N-pyrrolidino)formylimino                        302 SO.sub.2 CH.sub.3 phenyl (N-pyrrolidino)formyl-N-                             (methanesulfamoyl)imino                                                     303 SO.sub.2 CH.sub.3 2-F-phenyl guanidino                                     304 SO.sub.2 CH.sub.3 2-F-phenyl 2-thiazolin-2-ylamine                         305 SO.sub.2 CH.sub.3 2-F-phenyl N-methyl-2-imidazolin-2-yl                    306 SO.sub.2 CH.sub.3 2-F-phenyl N-methyl-1,4,5,6-                                tetrahydropyrimid-2-yl                                                      307 SO.sub.2 CH.sub.3 2-F-phenyl N-methylimidazol-2-ylthio                     308 SO.sub.2 CH.sub.3 2-F-phenyl t-butoxycarbonylamine                         309 SO.sub.2 CH.sub.3 2-F-phenyl (N-pyrrolidino)formylimino                    310 SO.sub.2 CH.sub.3 2-F-phenyl (N-pyrrolidino)formyl-N-                         (methanesulfamoyl)imino                                                     311 SO.sub.2 CH.sub.3 2-CH.sub.3 O-phenyl (N-pyrrolidino)formylimino                                     312 SO.sub.2 CH.sub.3 2-CH.sub.3 O-phenyl                                     (N-pyrrolidino)formyl-N-                                 (methanesulfamoyl)imino                                                     313 NHSO.sub.2 CH.sub.3 phenyl 2-((Me).sub.2 N-methyl)phenyl                   314 NHSO.sub.2 CH.sub.3 phenyl 2-((Me)NH-methyl)phenyl                         315 NHSO.sub.2 CH.sub.3 phenyl 2-(H.sub.2 N-methyl)phenyl                      316 NHSO.sub.2 CH.sub.3 phenyl 2-HOCH.sub.2 -phenyl                            317 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-((Me).sub.2 N-methyl)phenyl                                         318 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-((Me)NH-m                                ethyl)phenyl                                          319 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(H.sub.2 N-methyl)phenyl                  320 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-HOCH.sub.2 -phenyl                        321 NHSO.sub.2 CH.sub.3 phenyl 2-methylimidazol-1-yl                           322 NHSO.sub.2 CH.sub.3 phenyl 2-ethylimidazol-1-yl                            323 NHSO.sub.2 CH.sub.3 phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                                      324 NHSO.sub.2 CH.sub.3 phenyl 2-CH.sub.3                                     SO.sub.2 -imidazol-1-yl                               325 NHSO.sub.2 CH.sub.3 phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                                       326 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-methylimi                                dazol-1-yl                                            327 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-ethylimidazol-1-yl                        328 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl        329 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                                    330 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-CH.sub.3                                 OCH.sub.2 -imidazol-1-yl                              331 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-methylimidazol-1-yl                      332 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-ethylimidazol-1-yl                       333 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl       334 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                                   335 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-CH.sub.3                                 OCH.sub.2 -imidazol-1-yl                             336 NHSO.sub.2 CH.sub.3 2-(Me).sub.2 N-phenyl 2-methylimidazol-1-yl                                      337 NHSO.sub.2 CH.sub.3 2-(Me).sub.2 N-phenyl                                 2-ethylimidazol-1-yl                                  338 NHSO.sub.2 CH.sub.3 2-(Me).sub.2 N-phenyl 2-((Me).sub.2 N-methyl)imi                                dazol-1-yl                                            339 NHSO.sub.2 CH.sub.3 2-(Me).sub.2 N-phenyl 2-CH.sub.3 SO.sub.2                                       -imidazol-1-yl                                        340 NHSO.sub.2 CH.sub.3 2-(Me).sub.2 N-phenyl 2-CH.sub.3 OCH.sub.2                                      -imidazol-1-yl                                        341 NHSO.sub.2 CH.sub.3 phenyl N-methylimidazol-2-yl                           342 NHSO.sub.2 CH.sub.3 phenyl 4-methylimidazol-5-yl                           343 NHSO.sub.2 CH.sub.3 phenyl 5-CF.sub.3 -pyrazol-1-yl                        344 NHSO.sub.2 CH.sub.3 2-F-phenyl N-methylimidazol-2-yl                       345 NHSO.sub.2 CH.sub.3 2-F-phenyl 4-methylimidazol-5-yl                       346 NHSO.sub.2 CH.sub.3 2-F-phenyl 5-CF.sub.3 -pyrazol-1-yl                    347 NHSO.sub.2 CH.sub.3 phenyl guanidino                                       348 NHSO.sub.2 CH.sub.3 phenyl 2-thiazolin-2-ylamine                           349 NHSO.sub.2 CH.sub.3 phenyl N-methyl-2-imidazolin-2-yl                      350 NHSO.sub.2 CH.sub.3 phenyl N-methyl-1,4,5,6-                                  tetrahydropyrimid-2-yl                                                      351 NHSO.sub.2 CH.sub.3 phenyl N-methylimidazol-2-ylthiol                      352 NHSO.sub.2 CH.sub.3 phenyl t-butoxycarbonylamine                           353 NHSO.sub.2 CH.sub.3 phenyl (N-pyrrolidino)formylimino                      354 NHSO.sub.2 CH.sub.3 phenyl (N-pyrrolidino)formyl-N-                           (methanesulfamoyl)imino                                                     355 NHSO.sub.2 CH.sub.3 2-F-phenyl guanidino                                   356 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-thiazolin-2-ylamine                       357 NHSO.sub.2 CH.sub.3 2-F-phenyl N-methyl-2-imidazolin-2-yl                  358 NHSO.sub.2 CH.sub.3 2-F-phenyl N-methyl-1,4,5,6-                              tetrahydropyrimid-2-yl                                                      359 NHSO.sub.2 CH.sub.3 2-F-phenyl N-methylimidazol-2-ylthio                   360 NHSO.sub.2 CH.sub.3 2-F-phenyl t-butoxycarbonylamine                       361 NHSO.sub.2 CH.sub.3 2-F-phenyl (N-pyrrolidino)formylimino                  362 NHSO.sub.2 CH.sub.3 2-F-phenyl (N-pyrrolidino)formyl-N-                       (methanesulfamoyl)imino                                                     363 NHSO.sub.2 CH.sub.3 2-CH.sub.3 O-phenyl (N-pyrrolidino)formylimino                                   364 NHSO.sub.2 CH.sub.3 2-CH.sub.3 O-phenyl                                   (N-pyrrolidino)formyl-N-                                 (methanesulfamoyl)imino                                                   ______________________________________                                    

                                      TABLE 4                                      __________________________________________________________________________       #STR120##                                                                    __________________________________________________________________________                                                 #STR121##                                                                      #STR122##                                                                     ##STR123##                          __________________________________________________________________________     a.sub.1                                                                           R = F, D = NH.sub.2                                                                              b.sub.1                                                                           R = F, D = NH.sub.2                                                                              c.sub.1                                                                           R = F, D = NH.sub.2                 a.sub.2 R = H, D = NH.sub.2 b.sub.2 R = H, D = NH.sub.2 c.sub.2 R = H,                                                    D = NH.sub.2                        a.sub.3 R = F, D = CH.sub.2 NH.sub.2 b.sub.3 R = F, D = CH.sub.2                                                          NH.sub.2 c.sub.3 R = F, D =                                                    CH.sub.2 NH.sub.2                   a.sub.4 R = H, D = CH.sub.2 NH.sub.2 b.sub.4 R = H, D = CH.sub.2                                                          NH.sub.2 c.sub.4 R = H, D =                                                    CH.sub.2 NH.sub.2                   a.sub.5 R = F, D = C(═NH)NH.sub.2 b.sub.5 R = F, D = C(═NH)NH.su                                                  b.2 c.sub.5 R = F, D =                                                         C(═NH)NH.sub.2                  a.sub.6 R = H, D = C(═NH)NH.sub.2 b.sub.6 R = H, D = C(═NH)NH.su                                                  b.2 c.sub.6 R = H, D =                                                         C(═NH)NH.sub.2                  a.sub.7 R = F, D = C(O)NH.sub.2 b.sub.7 R = F, D = C(O)NH.sub.2 c.sub.7                                                   R = F, D = C(O)NH.sub.2                                                         a.sub.8 R = H, D = C(O)NH.su                                                  b.2 b.sub.8 R = H, D =                                                         C(O)NH.sub.2 c.sub.8 R = H,                                                    D = C(O)NH.sub.2                  __________________________________________________________________________                                                 #STR124##                                                                      #STR125##                                                                     ##STR126##                          __________________________________________________________________________     d.sub.1                                                                           R = F, D = NH.sub.2                                                                              e.sub.1                                                                           R = F, D = NH.sub.2                                                                              f.sub.1                                                                           R = F, D = NH.sub.2                 d.sub.2 R = H, D = NH.sub.2 e.sub.2 R = H, D = NH.sub.2 f.sub.2 R = H,                                                    D = NH.sub.2                        d.sub.3 R = F, D = CH.sub.2 NH.sub.2 e.sub.3 R = F, D = CH.sub.2                                                          NH.sub.2 f.sub.3 R = F, D =                                                    CH.sub.2 NH.sub.2                   d.sub.4 R = H, D = CH.sub.2 NH.sub.2 e.sub.4 R = H, D = CH.sub.2                                                          NH.sub.2 f.sub.4 R = H, D =                                                    CH.sub.2 NH.sub.2                   d.sub.5 R = F, D = C(═NH)NH.sub.2 e.sub.5 R = F, D = C(═NH)NH.su                                                  b.2 f.sub.5 R = F, D =                                                         C(═NH)NH.sub.2                  d.sub.6 R = H, D = C(═NH)NH.sub.2 e.sub.6 R = H, D = C(═NH)NH.su                                                  b.2 f.sub.6 R = H, D =                                                         C(═NH)NH.sub.2                  d.sub.7 R = F, D = C(O)NH.sub.2 e.sub.7 R = F, D = C(O)NH.sub.2 f.sub.7                                                   R = F, D = C(O)NH.sub.2                                                         d.sub.8 R = H, D = C(O)NH.su                                                  b.2 e.sub.8 R = H, D =                                                         C(O)NH.sub.2 f.sub.8 R = H,                                                    D = C(O)NH.sub.2                  __________________________________________________________________________                                                 #STR127##                                                                      #STR128##                                                                     ##STR129##                          __________________________________________________________________________     g.sub.1                                                                           R = F, D = NH.sub.2                                                                              h.sub.1                                                                           R = F, D = NH.sub.2                                                                              i.sub.1                                                                           R = F, D = NH.sub.2                 g.sub.2 R = H, D = NH.sub.2 h.sub.2 R = H, D = NH.sub.2 i.sub.2 R = H,                                                    D = NH.sub.2                        g.sub.3 R = F, D = CH.sub.2 NH.sub.2 h.sub.3 R = F, D = CH.sub.2                                                          NH.sub.2 i.sub.3 R = F, D =                                                    CH.sub.2 NH.sub.2                   g.sub.4 R = H, D = CH.sub.2 NH.sub.2 h.sub.4 R = H, D = CH.sub.2                                                          NH.sub.2 i.sub.4 R = H, D =                                                    CH.sub.2 NH.sub.2                   g.sub.5 R = F, D = C(═NH)NH.sub.2 h.sub.5 R = F, D = C(═NH)NH.su                                                  b.2 i.sub.5 R = F, D =                                                         C(═NH)NH.sub.2                  g.sub.6 R = H, D = C(═NH)NH.sub.2 h.sub.6 R = H, D = C(═NH)NH.su                                                  b.2 i.sub.6 R = H, D =                                                         C(═NH)NH.sub.2                  g.sub.7 R = F, D = C(O)NH.sub.2 h.sub.7 R = F, D = C(O)NH.sub.2 i.sub.7                                                   R = F, D = C(O)NH.sub.2                                                         g.sub.8 R = H, D = C(O)NH.su                                                  b.2 h.sub.8 R = H, D =                                                         C(O)NH.sub.2 i.sub.8 R = H,                                                    D = C(O)NH.sub.2                  __________________________________________________________________________                                                 #STR130##                                                                      #STR131##                                                                     ##STR132##                          __________________________________________________________________________     j.sub.1                                                                           R = F, D = NH.sub.2                                                                              k.sub.1                                                                           R = F, D = NH.sub.2                                                                              l.sub.1                                                                           R = F, D = NH.sub.2                 j.sub.2 R = H, D = NH.sub.2 k.sub.2 R = H, D = NH.sub.2 l.sub.2 R = H,                                                    D = NH.sub.2                        j.sub.3 R = F, D = CH.sub.2 NH.sub.2 k.sub.3 R = F, D = CH.sub.2                                                          NH.sub.2 l.sub.3 R = F, D =                                                    CH.sub.2 NH.sub.2                   j.sub.4 R = H, D = CH.sub.2 NH.sub.2 k.sub.4 R = H, D = CH.sub.2                                                          NH.sub.2 l.sub.4 R = H, D =                                                    CH.sub.2 NH.sub.2                   j.sub.5 R = F, D = C(═NH)NH.sub.2 k.sub.5 R = F, D = C(═NH)NH.su                                                  b.2 l.sub.5 R = F, D =                                                         C(═NH)NH.sub.2                  j.sub.6 R = H, D = C(═NH)NH.sub.2 k.sub.6 R = H, D = C(═NH)NH.su                                                  b.2 l.sub.6 R = H, D =                                                         C(═NH)NH.sub.2                  j.sub.7 R = F, D = C(O)NH.sub.2 k.sub.7 R = F, D = C(O)NH.sub.2 l.sub.7                                                   R = F, D = C(O)NH.sub.2                                                         j.sub.8 R = H, D = C(O)NH.su                                                  b.2 k.sub.8 R = H, D =                                                         C(O)NH.sub.2 l.sub.8 R = H,                                                    D = C(O)NH.sub.2                  __________________________________________________________________________                                                 #STR133##                                                                      #STR134##                                                                     ##STR135##                          __________________________________________________________________________     m.sub.1                                                                           R = F, D = NH.sub.2                                                                              n.sub.1                                                                           R = F, D = NH.sub.2                                                                              o.sub.1                                                                           R = F, D = NH.sub.2                 m.sub.2 R = H, D = NH.sub.2 n.sub.2 R = H, D = NH.sub.2 o.sub.2 R = H,                                                    D = NH.sub.2                        m.sub.3 R = F, D = CH.sub.2 NH.sub.2 n.sub.3 R = F, D = CH.sub.2                                                          NH.sub.2 o.sub.3 R = F, D =                                                    CH.sub.2 NH.sub.2                   m.sub.4 R = H, D = CH.sub.2 NH.sub.2 n.sub.4 R = H, D = CH.sub.2                                                          NH.sub.2 o.sub.4 R = H, D =                                                    CH.sub.2 NH.sub.2                   m.sub.5 R = F, D = C(═NH)NH.sub.2 n.sub.5 R = F, D = C(═NH)NH.su                                                  b.2 o.sub.5 R = F, D =                                                         C(═NH)NH.sub.2                  m.sub.6 R = H, D = C(═NH)NH.sub.2 n.sub.6 R = H, D = C(═NH)NH.su                                                  b.2 o.sub.6 R = H, D =                                                         C(═NH)NH.sub.2                  m.sub.7 R = F, D = C(O)NH.sub.2 n.sub.7 R = F, D = C(O)NH.sub.2 o.sub.7                                                   R = F, D = C(O)NH.sub.2                                                         m.sub.8 R = H, D = C(O)NH.su                                                  b.2 n.sub.8 R = H, D =                                                         C(O)NH.sub.2 o.sub.8 R = H,                                                    D = C(O)NH.sub.2                  __________________________________________________________________________                                                 #STR136##                                                                      #STR137##                                                                     ##STR138##                          __________________________________________________________________________     p.sub.1                                                                           R = F, D = NH.sub.2                                                                              q.sub.1                                                                           R = F, D = NH.sub.2                                                                              r.sub.1                                                                           R = F, D = NH.sub.2                 p.sub.2 R = Cl, D = NH.sub.2 q.sub.2 R = Cl, D = NH.sub.2 r.sub.2 R =                                                     Cl, D = NH.sub.2                    p.sub.3 R = OMe, D = NH.sub.2 q.sub.3 R = OMe, D = NH.sub.2 r.sub.3 R =                                                   OMe, D = NH.sub.2                   p.sub.4 R = F, D = CH.sub.2 NH.sub.2 q.sub.4 R = F, D = CH.sub.2                                                          NH.sub.2 r.sub.4 R = F, D =                                                    CH.sub.2 NH.sub.2                   p.sub.5 R = Cl, D = CH.sub.2 NH.sub.2 q.sub.5 R = Cl, D = CH.sub.2                                                        NH.sub.2 r.sub.5 R = Cl, D =                                                   CH.sub.2 NH.sub.2                   p.sub.6 R = OMe, D = CH.sub.2 NH.sub.2 q.sub.6 R = OMe, D = CH.sub.2                                                      NH.sub.2 r.sub.6 R = OMe, D                                                    = CH.sub.2 NH.sub.2                 p.sub.7 R = F, D = C(═NH)NH.sub.2 q.sub.7 R = F, D = C(═NH)NH.su                                                  b.2 r.sub.7 R = F, D =                                                         C(═NH)NH.sub.2                  p.sub.8 R = Cl, D = C(═NH)NH.sub.2 q.sub.8 R = Cl, D = C(═NH)NH.                                                  sub.2 r.sub.8 R = Cl, D =                                                      C(═NH)NH.sub.2                  p.sub.9 R = OMe, D = C(═NH)NH.sub.2 q.sub.9 R = OMe, D = C(═NH)N                                                  H.sub.2 r.sub.9 R = OMe, D =                                                   C(═NH)NH.sub.2                  p.sub.10 R = F, D = C(O)NH.sub.2 q.sub.10 R = F, D = C(O)NH.sub.2                                                         r.sub.10 R = F, D = C(O)NH.su                                                  b.2                                 p.sub.11 R = Cl, D = C(O)NH.sub.2 q.sub.11 R = Cl, D = C(O)NH.sub.2                                                       r.sub.11 R = Cl, D =                                                           C(O)NH.sub.2                        p.sub.12 R = OMe, D = C(O)NH.sub.2 q.sub.12 R = OMe, D = C(O)NH.sub.2                                                     r.sub.12 R = OMe, D =                                                          C(O)NH.sub.2                      __________________________________________________________________________                                                 #STR139##                                                                      #STR140##                                                                     ##STR141##                          __________________________________________________________________________     s.sub.1                                                                           R = F, D = NH.sub.2                                                                              t.sub.1                                                                           R = F, D = NH.sub.2                                                                              u.sub.1                                                                           R = F, D = NH.sub.2                 s.sub.2 R = Cl, D = NH.sub.2 t.sub.2 R = Cl, D = NH.sub.2 u.sub.2 R =                                                     Cl, D = NH.sub.2                    s.sub.3 R = OMe, D = NH.sub.2 t.sub.3 R = OMe, D = NH.sub.2 u.sub.3 R =                                                   OMe, D = NH.sub.2                   s.sub.4 R = F, D = CH.sub.2 NH.sub.2 t.sub.4 R = F, D = CH.sub.2                                                          NH.sub.2 u.sub.4 R = F, D =                                                    CH.sub.2 NH.sub.2                   s.sub.5 R = Cl, D = CH.sub.2 NH.sub.2 t.sub.5 R = Cl, D = CH.sub.2                                                        NH.sub.2 u.sub.5 R = Cl, D =                                                   CH.sub.2 NH.sub.2                   s.sub.6 R = OMe, D = CH.sub.2 NH.sub.2 t.sub.6 R = OMe, D = CH.sub.2                                                      NH.sub.2 u.sub.6 R = OMe, D                                                    = CH.sub.2 NH.sub.2                 s.sub.7 R = F, D = C(═NH)NH.sub.2 t.sub.7 R = F, D = C(═NH)NH.su                                                  b.2 u.sub.7 R = F, D =                                                         C(═NH)NH.sub.2                  s.sub.8 R = Cl, D = C(═NH)NH.sub.2 t.sub.8 R = Cl, D = C(═NH)NH.                                                  sub.2 u.sub.8 R = Cl, D =                                                      C(═NH)NH.sub.2                  s.sub.9 R = OMe, D = C(═NH)NH.sub.2 t.sub.9 R = OMe, D = C(═NH)N                                                  H.sub.2 u.sub.9 R = OMe, D =                                                   C(═NH)NH.sub.2                  s.sub.10 R = F, D = C(O)NH.sub.2 t.sub.10 R = F, D = C(O)NH.sub.2                                                         u.sub.10 R = F, D = C(O)NH.su                                                  b.2                                 s.sub.11 R = Cl, D = C(O)NH.sub.2 t.sub.11 R = Cl, D = C(O)NH.sub.2                                                       u.sub.11 R = Cl, D =                                                           C(O)NH.sub.2                        s.sub.12 R = OMe, D = C(O)NH.sub.2 t.sub.12 R = OMe, D = C(O)NH.sub.2                                                     u.sub.12 R = OMe, D =                                                          C(O)NH.sub.2                      __________________________________________________________________________                                                 #STR142##                                                                      #STR143##                                                                     ##STR144##                          __________________________________________________________________________     v.sub.1                                                                           R = F, D = NH.sub.2                                                                              w.sub.1                                                                           R = F, D = NH.sub.2                                                                              x.sub.1                                                                           R = F, D = NH.sub.2                 v.sub.2 R = Cl, D = NH.sub.2 w.sub.2 R = Cl, D = NH.sub.2 x.sub.2 R =                                                     Cl, D = NH.sub.2                    v.sub.3 R = OMe, D = NH.sub.2 w.sub.3 R = OMe, D = NH.sub.2 x.sub.3 R =                                                   OMe, D = NH.sub.2                   v.sub.4 R = F, D = CH.sub.2 NH.sub.2 w.sub.4 R = F, D = CH.sub.2                                                          NH.sub.2 x.sub.4 R = F, D =                                                    CH.sub.2 NH.sub.2                   v.sub.5 R = Cl, D = CH.sub.2 NH.sub.2 w.sub.5 R = Cl, D = CH.sub.2                                                        NH.sub.2 x.sub.5 R = Cl, D =                                                   CH.sub.2 NH.sub.2                   v.sub.6 R = OMe, D = CH.sub.2 NH.sub.2 w.sub.6 R = OMe, D = CH.sub.2                                                      NH.sub.2 x.sub.6 R = OMe, D                                                    = CH.sub.2 NH.sub.2                 v.sub.7 R = F, D = C(═NH)NH.sub.2 w.sub.7 R = F, D = C(═NH)NH.su                                                  b.2 x.sub.7 R = F, D =                                                         C(═NH)NH.sub.2                  v.sub.8 R = Cl, D = C(═NH)NH.sub.2 w.sub.8 R = Cl, D = C(═NH)NH.                                                  sub.2 x.sub.8 R = Cl, D =                                                      C(═NH)NH.sub.2                  v.sub.9 R = OMe, D = C(═NH)NH.sub.2 w.sub.9 R = OMe, D = C(═NH)N                                                  H.sub.2 x.sub.9 R = OMe, D =                                                   C(═NH)NH.sub.2                  v.sub.10 R = F, D = C(O)NH.sub.2 w.sub.10 R = F, D = C(O)NH.sub.2                                                         x.sub.10 R = F, D = C(O)NH.su                                                  b.2                                 v.sub.11 R = Cl, D = C(O)NH.sub.2 w.sub.11 R = Cl, D = C(O)NH.sub.2                                                       x.sub.11 R = Cl, D =                                                           C(O)NH.sub.2                        v.sub.12 R = OMe, D = C(O)NH.sub.2 w.sub.12 R = OMe, D = C(O)NH.sub.2                                                     x.sub.12 R = OMe, D =                                                          C(O)NH.sub.2                      __________________________________________________________________________                                                 #STR145##                                                                      #STR146##                                                                     ##STR147##                          __________________________________________________________________________     y.sub.1                                                                           R = F, D = NH.sub.2                                                                              z.sub.1                                                                           R = F, D = NH.sub.2                                                                              aa.sub.1                                                                          R = F, D = NH.sub.2                 y.sub.2 R = Cl, D = NH.sub.2 z.sub.2 R = Cl, D = NH.sub.2 aa.sub.2 R =                                                    Cl, D = NH.sub.2                    y.sub.3 R = OMe, D = NH.sub.2 z.sub.3 R = OMe, D = NH.sub.2 aa.sub.3 R                                                    = OMe, D = NH.sub.2                 y.sub.4 R = F, D = CH.sub.2 NH.sub.2 z.sub.4 R = F, D = CH.sub.2                                                          NH.sub.2 aa.sub.4 R = F, D =                                                   CH.sub.2 NH.sub.2                   y.sub.5 R = Cl, D = CH.sub.2 NH.sub.2 z.sub.5 R = Cl, D = CH.sub.2                                                        NH.sub.2 aa.sub.5 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 y.sub.6 R = OMe, D = CH.sub.2 NH.sub.2 z.sub.6 R = OMe, D = CH.sub.2                                                      NH.sub.2 aa.sub.6 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 y.sub.7 R = F, D = C(═NH)NH.sub.2 z.sub.7 R = F, D = C(═NH)NH.su                                                  b.2 aa.sub.7 R = F, D =                                                        C(═NH)NH.sub.2                  y.sub.8 R = Cl, D = C(═NH)NH.sub.2 z.sub.8 R = Cl, D = C(═NH)NH.                                                  sub.2 aa.sub.8 R = Cl, D =                                                     C(═NH)NH.sub.2                  y.sub.9 R = OMe, D = C(═NH)NH.sub.2 z.sub.9 R = OMe, D = C(═NH)N                                                  H.sub.2 aa.sub.9 R = OMe, D                                                    = C(═NH)NH.sub.2                                                            y.sub.10 R = F, D =                                                           C(O)NH.sub.2 z.sub.10 R = F,                                                   D = C(O)NH.sub.2 aa.sub.10 R                                                   = F, D = C(O)NH.sub.2                                                           y.sub.11 R = Cl, D =                                                          C(O)NH.sub.2 z.sub.11 R =                                                      Cl, D = C(O)NH.sub.2                                                           aa.sub.11 R = Cl, D =                                                          C(O)NH.sub.2                        y.sub.12 R = OMe, D = C(O)NH.sub.2 z.sub.12 R = OMe, D = C(O)NH.sub.2                                                     aa.sub.12 R = OMe, D =                                                         C(O)NH.sub.2                      __________________________________________________________________________                                                 #STR148##                                                                      #STR149##                                                                     ##STR150##                          __________________________________________________________________________     bb.sub.1                                                                          R = F, D = NH.sub.2                                                                              cc.sub.1                                                                          R = F, D = NH.sub.2                                                                              dd.sub.1                                                                          R = F, D = NH.sub.2                 bb.sub.2 R = Cl, D = NH.sub.2 cc.sub.2 R = Cl, D = NH.sub.2 dd.sub.2 R                                                    = Cl, D = NH.sub.2                  bb.sub.3 R = OMe, D = NH.sub.2 cc.sub.3 R = OMe, D = NH.sub.2 dd.sub.3                                                    R = OMe, D = NH.sub.2                                                           bb.sub.4 R = F, D =                                                           CH.sub.2 NH.sub.2 cc.sub.4 R                                                   = F, D = CH.sub.2 NH.sub.2                                                     dd.sub.4 R = F, D = CH.sub.2                                                   NH.sub.2                            bb.sub.5 R = Cl, D = CH.sub.2 NH.sub.2 cc.sub.5 R = Cl, D = CH.sub.2                                                      NH.sub.2 dd.sub.5 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 bb.sub.6 R = OMe, D = CH.sub.2 NH.sub.2 cc.sub.6 R = OMe, D = CH.sub.2                                                    NH.sub.2 dd.sub.6 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 bb.sub.7 R = F, D = C(═NH)NH.sub.2 cc.sub.7 R = F, D = C(═NH)NH.                                                  sub.2 dd.sub.7 R = F, D =                                                      C(═NH)NH.sub.2                  bb.sub.8 R = Cl, D = C(═NH)NH.sub.2 cc.sub.8 R = Cl, D = C(═NH)N                                                  H.sub.2 dd.sub.8 R = Cl, D =                                                   C(═NH)NH.sub.2                  bb.sub.9 R = OMe, D = C(═NH)NH.sub.2 cc.sub.9 R = OMe, D = C(═NH                                                  )NH.sub.2 dd.sub.9 R = OMe,                                                    D = C(═NH)NH.sub.2                                                          bb.sub.10 R = F, D =                                                          C(O)NH.sub.2 cc.sub.10 R =                                                     F, D = C(O)NH.sub.2 dd.sub.10                                                   R = F, D = C(O)NH.sub.2                                                        bb.sub.11 R = Cl, D =                                                         C(O)NH.sub.2 cc.sub.11 R =                                                     Cl, D = C(O)NH.sub.2                                                           dd.sub.11 R = Cl, D =                                                          C(O)NH.sub.2                        bb.sub.12 R = OMe, D = C(O)NH.sub.2 cc.sub.12 R = OMe, D = C(O)NH.sub.2                                                   dd.sub.12 R = OMe, D =                                                         C(O)NH.sub.2                      __________________________________________________________________________                                                 #STR151##                                                                      #STR152##                                                                     ##STR153##                          __________________________________________________________________________     ee.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     ff.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     gg.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2        ee.sub.2 R = Cl, D = CH.sub.2 NH.sub.2 ff.sub.2 R = Cl, D = CH.sub.2                                                      NH.sub.2 gg.sub.2 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 ee.sub.3 R = OMe, D = CH.sub.2 NH.sub.2 ff.sub.3 R = OMe, D = CH.sub.2                                                    NH.sub.2 gg.sub.3 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 ee.sub.4 R = CH.sub.2 NH.sub.2, ff.sub.4 R = CH.sub.2 NH.sub.2,                                                           gg.sub.4 R = CH.sub.2                                                          NH.sub.2,                            D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2         __________________________________________________________________________                                                 #STR154##                                                                      #STR155##                                                                     ##STR156##                          __________________________________________________________________________     hh.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     ii.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     jj.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2        hh.sub.2 R = Cl, D = CH.sub.2 NH.sub.2 ii.sub.2 R = Cl, D = CH.sub.2                                                      NH.sub.2 jj.sub.2 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 hh.sub.3 R = OMe, D = CH.sub.2 NH.sub.2 ii.sub.3 R = OMe, D = CH.sub.2                                                    NH.sub.2 jj.sub.3 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 hh.sub.4 R = CH.sub.2 NH.sub.2, ii.sub.4 R = CH.sub.2 NH.sub.2,                                                           jj.sub.4 R = CH.sub.2                                                          NH.sub.2,                            D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2         __________________________________________________________________________                                                 #STR157##                                                                      #STR158##                                                                     ##STR159##                          __________________________________________________________________________     kk.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     ll.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     mm.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2        kk.sub.2 R = Cl, D = CH.sub.2 NH.sub.2 ll.sub.2 R = Cl, D = CH.sub.2                                                      NH.sub.2 mm.sub.2 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 kk.sub.3 R = OMe, D = CH.sub.2 NH.sub.2 ll.sub.3 R = OMe, D = CH.sub.2                                                    NH.sub.2 mm.sub.3 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 kk.sub.4 R = CH.sub.2 NH.sub.2, ll.sub.4 R = CH.sub.2 NH.sub.2,                                                           mm.sub.4 R = CH.sub.2                                                          NH.sub.2,                            D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2         __________________________________________________________________________                                                 #STR160##                                                                      #STR161##                                                                     ##STR162##                          __________________________________________________________________________     nn.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     oo.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     pp.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2        nn.sub.2 R = Cl, D = CH.sub.2 NH.sub.2 oo.sub.2 R = Cl, D = CH.sub.2                                                      NH.sub.2 pp.sub.2 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 nn.sub.3 R = OMe, D = CH.sub.2 NH.sub.2 oo.sub.3 R = OMe, D = CH.sub.2                                                    NH.sub.2 pp.sub.3 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 nn.sub.4 R = CH.sub.2 NH.sub.2, oo.sub.4 R = CH.sub.2 NH.sub.2,                                                           pp.sub.4 R = CH.sub.2                                                          NH.sub.2,                            D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2         __________________________________________________________________________                                                 #STR163##                                                                      #STR164##                                                                     ##STR165##                          __________________________________________________________________________     qq.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     rr.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     ss.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2        qq.sub.2 R = Cl, D = CH.sub.2 NH.sub.2 rr.sub.2 R = Cl, D = CH.sub.2                                                      NH.sub.2 ss.sub.2 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 qq.sub.3 R = OMe, D = CH.sub.2 NH.sub.2 rr.sub.3 R = OMe, D = CH.sub.2                                                    NH.sub.2 ss.sub.3 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 qq.sub.4 R = CH.sub.2 NH.sub.2, rr.sub.4 R = CH.sub.2 NH.sub.2,                                                           ss.sub.4 R = CH.sub.2                                                          NH.sub.2,                            D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2         __________________________________________________________________________

    ______________________________________                                         Ex#  R.sup.1b  A          B                                                    ______________________________________                                         1    H         phenyl     2-(aminosulfonyl)phenyl                                2 H phenyl 2-(methylaminosulfonyl)phenyl                                       3 H phenyl 1-pyrrolidinocarbonyl                                               4 H phenyl 2-(methylsulfonyl)phenyl                                            5 H phenyl 4-morpholino                                                        6 H phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                7 H phenyl 4-morpholinocarbonyl                                                8 H 2-pyridyl 2-(aminosulfonyl)phenyl                                          9 H 2-pyridyl 2-(methylaminosulfonyl)phenyl                                    10 H 2-pyridyl 1-pyrrolidinocarbonyl                                           11 H 2-pyridyl 2-(methylsulfonyl)phenyl                                        12 H 2-pyridyl 4-morpholino                                                    13 H 2-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                            14 H 2-pyridyl 4-morpholinocarbonyl                                            15 H 3-pyridyl 2-(aminosulfonyl)phenyl                                         16 H 3-pyridyl 2-(methylaminosulfonyl)phenyl                                   17 H 3-pyridyl 1-pyrrolidinocarbonyl                                           18 H 3-pyridyl 2-(methylsulfonyl)phenyl                                        19 H 3-pyridyl 4-morpholino                                                    20 H 3-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                            21 H 3-pyridyl 4-morpholinocarbonyl                                            22 H 2-pyrimidyl 2-(aminosulfonyl)phenyl                                       23 H 2-pyrimidyl 2-(methylaminosulfonyl)phenyl                                 24 H 2-pyrimidyl 1-pyrrolidinocarbonyl                                         25 H 2-pyrimidyl 2-(methylsulfonyl)phenyl                                      26 H 2-pyrimidyl 4-morpholino                                                  27 H 2-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                          28 H 2-pyrimidyl 4-morpholinocarbonyl                                          29 H 5-pyrimidyl 2-(aminosulfonyl)phenyl                                       30 H 5-pyrimidyl 2-(methylaminosulfonyl)phenyl                                 31 H 5-pyrimidyl 1-pyrrolidinocarbonyl                                         32 H 5-pyrimidyl 2-(methylsulfonyl)phenyl                                      33 H 5-pyrimidyl 4-morpholino                                                  34 H 5-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                          35 H 5-pyrimidyl 4-morpholinocarbonyl                                          36 H 2-Cl-phenyl 2-(aminosulfonyl)phenyl                                       37 H 2-Cl-phenyl 2-(methylaminosulfonyl)phenyl                                 38 H 2-Cl-phenyl 1-pyrrolidinocarbonyl                                         39 H 2-Cl-phenyl 2-(methylsulfonyl)phenyl                                      40 H 2-Cl-phenyl 4-morpholino                                                  41 H 2-Cl-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                          42 H 2-Cl-phenyl 4-morpholinocarbonyl                                          43 H 2-F-phenyl 2-(aminosulfonyl)phenyl                                        44 H 2-F-phenyl 2-(methylaminosulfonyl)phenyl                                  45 H 2-F-phenyl 1-pyrrolidinocarbonyl                                          46 H 2-F-phenyl 2-(methylsulfonyl)phenyl                                       47 H 2-F-phenyl 4-morpholino                                                   48 H 2-F-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                           49 H 2-F-phenyl 4-morpholinocarbonyl                                           50 H 2,5-diF-phenyl 2-(aminosulfonyl)phenyl                                    51 H 2,5-diF-phenyl 2-(methylaminosulfonyl)phenyl                              52 H 2,5-diF-phenyl 1-pyrrolidinocarbonyl                                      53 H 2,5-diF-phenyl 2-(methylsulfonyl)phenyl                                   54 H 2,5-diF-phenyl 4-morpholino                                               55 H 2,5-diF-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                       56 H 2,5-diF-phenyl 4-morpholinocarbonyl                                       57 --CN phenyl 2-(aminosulfonyl)phenyl                                         58 --CN phenyl 2-(methylaminosulfonyl)phenyl                                   59 --CN phenyl 1-pyrrolidinocarbonyl                                           60 --CN phenyl 2-(methylsulfonyl)phenyl                                        61 --CN phenyl 4-morpholino                                                    62 --CN phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                            63 --CN phenyl 4-morpholinocarbonyl                                            64 --CN 2-pyridyl 2-(aminosulfonyl)phenyl                                      65 --CN 2-pyridyl 2-(methylaminosulfonyl)phenyl                                66 --CN 2-pyridyl 1-pyrrolidinocarbonyl                                        67 --CN 2-pyridyl 2-(methylsulfonyl)phenyl                                     68 --CN 2-pyridyl 4-morpholino                                                 69 --CN 2-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                         70 --CN 2-pyridyl 4-morpholinocarbonyl                                         71 --CN 3-pyridyl 2-(aminosulfonyl)phenyl                                      72 --CN 3-pyridyl 2-(methylaminosulfonyl)phenyl                                73 --CN 3-pyridyl 1-pyrrolidinocarbonyl                                        74 --CN 3-pyridyl 2-(methylsulfonyl)phenyl                                     75 --CN 3-pyridyl 4-morpholino                                                 76 --CN 3-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                         77 --CN 3-pyridyl 4-morpholinocarbonyl                                         78 --CN 2-pyrimidyl 2-(aminosulfonyl)phenyl                                    79 --CN 2-pyrimidyl 2-(methylaminosulfonyl)phenyl                              80 --CN 2-pyrimidyl 1-pyrrolidinocarbonyl                                      81 --CN 2-pyrimidyl 2-(methylsulfonyl)phenyl                                   82 --CN 2-pyrimidyl 4-morpholino                                               83 --CN 2-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                       84 --CN 2-pyrimidyl 4-morpholinocarbonyl                                       85 --CN 5-pyrimidyl 2-(aminosulfonyl)phenyl                                    86 --CN 5-pyrimidyl 2-(methylaminosulfonyl)phenyl                              87 --CN 5-pyrimidyl 1-pyrrolidinocarbonyl                                      88 --CN 5-pyrimidyl 2-(methylsulfonyl)phenyl                                   89 --CN 5-pyrimidyl 4-morpholino                                               90 --CN 5-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                       91 --CN 5-pyrimidyl 4-morpholinocarbonyl                                       92 --CN 2-Cl-phenyl 2-(aminosulfonyl)phenyl                                    93 --CN 2-Cl-phenyl 2-(methylaminosulfonyl)phenyl                              94 --CN 2-Cl-phenyl 1-pyrrolidinocarbonyl                                      95 --CN 2-Cl-phenyl 2-(methylsulfonyl)phenyl                                   96 --CN 2-Cl-phenyl 4-morpholino                                               97 --CN 2-Cl-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                       98 --CN 2-Cl-phenyl 4-morpholinocarbonyl                                       99 --CN 2-F-phenyl 2-(aminosulfonyl)phenyl                                     100 --CN 2-F-phenyl 2-(methylaminosulfonyl)phenyl                              101 --CN 2-F-phenyl 1-pyrrolidinocarbonyl                                      102 --CN 2-F-phenyl 2-(methylsulfonyl)phenyl                                   103 --CN 2-F-phenyl 4-morpholino                                               104 --CN 2-F-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                       105 --CN 2-F-phenyl 4-morpholinocarbonyl                                       106 --CN 2,5-diF-phenyl 2-(aminosulfonyl)phenyl                                107 --CN 2,5-diF-phenyl 2-(methylaminosulfonyl)phenyl                          108 --CN 2,5-diF-phenyl 1-pyrrolidinocarbonyl                                  109 --CN 2,5-diF-phenyl 2-(methylsulfonyl)phenyl                               110 --CN 2,5-diF-phenyl 4-morpholino                                           111 --CN 2,5-diF-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                   112 --CN 2,5-diF-phenyl 4-morpholinocarbonyl                                   113 CF.sub.3  phenyl 2-(aminosulfonyl)phenyl                                   114 CF.sub.3  phenyl 2-(methylaminosulfonyl)phenyl                             115 CF.sub.3  phenyl 1-pyrrolidinocarbonyl                                     116 CF.sub.3  phenyl 2-(methylsulfonyl)phenyl                                  117 CF.sub.3  phenyl 4-morpholino                                              118 CF.sub.3  phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                      119 CF.sub.3  phenyl 4-morpholinocarbonyl                                      120 CF.sub.3  2-pyridyl 2-(aminosulfonyl)phenyl                                121 CF.sub.3  2-pyridyl 2-(methylaminosulfonyl)phenyl                          122 CF.sub.3  2-pyridyl 1-pyrrolidinocarbonyl                                  123 CF.sub.3  2-pyridyl 2-(methylsulfonyl)phenyl                               124 CF.sub.3  2-pyridyl 4-morpholino                                           125 CF.sub.3  2-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                   126 CF.sub.3  2-pyridyl 4-morpholinocarbonyl                                   127 CF.sub.3  3-pyridyl 2-(aminosulfonyl)phenyl                                128 CF.sub.3  3-pyridyl 2-(methylaminosulfonyl)phenyl                          129 CF.sub.3  3-pyridyl 1-pyrrolidinocarbonyl                                  130 CF.sub.3  3-pyridyl 2-(methylsulfonyl)phenyl                               131 CF.sub.3  3-pyridyl 4-morpholino                                           132 CF.sub.3  3-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                   133 CF.sub.3  3-pyridyl 4-morpholinocarbonyl                                   134 CF.sub.3  2-pyrimidyl 2-(aminosulfonyl)phenyl                              135 CF.sub.3  2-pyrimidyl 2-(methylaminosulfonyl)phenyl                        136 CF.sub.3  2-pyrimidyl 1-pyrrolidinocarbonyl                                137 CF.sub.3  2-pyrimidyl 2-(methylsulfonyl)phenyl                             138 CF.sub.3  2-pyrimidyl 4-morpholino                                         139 CF.sub.3  2-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                 140 CF.sub.3  2-pyrimidyl 4-morpholinocarbonyl                                 141 CF.sub.3  5-pyrimidyl 2-(aminosulfonyl)phenyl                              142 CF.sub.3  5-pyrimidyl 2-(methylaminosulfonyl)phenyl                        143 CF.sub.3  5-pyrimidyl 1-pyrrolidinocarbonyl                                144 CF.sub.3  5-pyrimidyl 2-(methylsulfonyl)phenyl                             145 CF.sub.3  5-pyrimidyl 4-morpholino                                         146 CF.sub.3  5-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                 147 CF.sub.3  5-pyrimidyl 4-morpholinocarbonyl                                 148 CF.sub.3  2-Cl-phenyl 2-(aminosulfonyl)phenyl                              149 CF.sub.3  2-Cl-phenyl 2-(methylaminosulfonyl)phenyl                        150 CF.sub.3  2-Cl-phenyl 1-pyrrolidinocarbonyl                                151 CF.sub.3  2-Cl-phenyl 2-(methylsulfonyl)phenyl                             152 CF.sub.3  2-Cl-phenyl 4-morpholino                                         153 CF.sub.3  2-Cl-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                 154 CF.sub.3  2-Cl-phenyl 4-morpholinocarbonyl                                 155 CF.sub.3  2-F-phenyl 2-(aminosulfonyl)phenyl                               156 CF.sub.3  2-F-phenyl 2-(methylaminosulfonyl)phenyl                         157 CF.sub.3  2-F-phenyl 1-pyrrolidinocarbonyl                                 158 CF.sub.3  2-F-phenyl 2-(methylsulfonyl)phenyl                              159 CF.sub.3  2-F-phenyl 4-morpholino                                          160 CF.sub.3  2-F-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                  161 CF.sub.3  2-F-phenyl 4-morpholinocarbonyl                                  162 CF.sub.3  2,5-diF-phenyl 2-(aminosulfonyl)phenyl                           163 CF.sub.3  2,5-diF-phenyl 2-(methylaminosulfonyl)phenyl                     164 CF.sub.3  2,5-diF-phenyl 1-pyrrolidinocarbonyl                             165 CF.sub.3  2,5-diF-phenyl 2-(methylsulfonyl)phenyl                          166 CF.sub.3  2,5-diF-phenyl 4-morpholino                                      167 CF.sub.3  2,5-diF-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                       168 CF.sub.3  2,5-diF-phenyl 4-morpholinocarbon                               yl                                                     169 CONH.sub.2 phenyl 2-(aminosulfonyl)phenyl                                  170 CONH.sub.2 phenyl 2-(methylaminosulfonyl)phenyl                            171 CONH.sub.2 phenyl 1-pyrrolidinocarbonyl                                    172 CONH.sub.2 phenyl 2-(methylsulfonyl)phenyl                                 173 CONH.sub.2 phenyl 4-morpholino                                             174 CONH.sub.2 phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                     175 CONH.sub.2 phenyl 4-morpholinocarbonyl                                     176 CONH.sub.2 2-pyridyl 2-(aminosulfonyl)phenyl                               177 CONH.sub.2 2-pyridyl 2-(methylaminosulfonyl)phenyl                         178 CONH.sub.2 2-pyridyl 1-pyrrolidinocarbonyl                                 179 CONH.sub.2 2-pyridyl 2-(methylsulfonyl)phenyl                              180 CONH.sub.2 2-pyridyl 4-morpholino                                          181 CONH.sub.2 2-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                  182 CONH.sub.2 2-pyridyl 4-morpholinocarbonyl                                  183 CONH.sub.2 3-pyridyl 2-(aminosulfonyl)phenyl                               184 CONH.sub.2 3-pyridyl 2-(methylaminosulfonyl)phenyl                         185 CONH.sub.2 3-pyridyl 1-pyrrolidinocarbonyl                                 186 CONH.sub.2 3-pyridyl 2-(methylsulfonyl)phenyl                              187 CONH.sub.2 3-pyridyl 4-morpholino                                          188 CONH.sub.2 3-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                  189 CONH.sub.2 3-pyridyl 4-morpholinocarbonyl                                  190 CONH.sub.2 2-pyrimidyl 2-(aminosulfonyl)phenyl                             191 CONH.sub.2 2-pyrimidyl 2-(methylaminosulfonyl)phenyl                       192 CONH.sub.2 2-pyrimidyl 1-pyrrolidinocarbonyl                               193 CONH.sub.2 2-pyrimidyl 2-(methylsulfonyl)phenyl                            194 CONH.sub.2 2-pyrimidyl 4-morpholino                                        195 CONH.sub.2 2-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                         196 CONH.sub.2 2-pyrimidyl 4-morpholinocarbonyl       197 CONH.sub.2 5-pyrimidyl 2-(aminosulfonyl)phenyl                             198 CONH.sub.2 5-pyrimidyl 2-(methylaminosulfonyl)phenyl                       199 CONH.sub.2 5-pyrimidyl 1-pyrrolidinocarbonyl                               200 CONH.sub.2 5-pyrimidyl 2-(methylsulfonyl)phenyl                            201 CONH.sub.2 5-pyrimidyl 4-morpholino                                        202 CONH.sub.2 5-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                         203 CONH.sub.2 5-pyrimidyl 4-morpholinocarbonyl       204 CONH.sub.2 2-Cl-phenyl 2-(aminosulfonyl)phenyl                             205 CONH.sub.2 2-Cl-phenyl 2-(methylaminosulfonyl)phenyl                       206 CONH.sub.2 2-Cl-phenyl 1-pyrrolidinocarbonyl                               207 CONH.sub.2 2-Cl-phenyl 2-(methylsulfonyl)phenyl                            208 CONH.sub.2 2-Cl-phenyl 4-morpholino                                        209 CONH.sub.2 2-Cl-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                         210 CONH.sub.2 2-Cl-phenyl 4-morpholinocarbonyl       211 CONH.sub.2 2-F-phenyl 2-(aminosulfonyl)phenyl                              212 CONH.sub.2 2-F-phenyl 2-(methylaminosulfonyl)phenyl                        213 CONH.sub.2 2-F-phenyl 1-pyrrolidinocarbonyl                                214 CONH.sub.2 2-F-phenyl 2-(methylsulfonyl)phenyl                             215 CONH.sub.2 2-F-phenyl 4-morpholino                                         216 CONH.sub.2 2-F-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                 217 CONH.sub.2 2-F-phenyl 4-morpholinocarbonyl                                 218 CONH.sub.2 2,5-diF-phenyl 2-(aminosulfonyl)phenyl                          219 CONH.sub.2 2,5-diF-phenyl 2-(methylaminosulfonyl)phenyl                    220 CONH.sub.2 2,5-diF-phenyl 1-pyrrolidinocarbonyl                            221 CONH.sub.2 2,5-diF-phenyl 2-(methylsulfonyl)phenyl                         222 CONH.sub.2 2,5-diF-phenyl 4-morpholino                                     223 CONH.sub.2 2,5-diF-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                      224 CONH.sub.2 2,5-diF-phenyl 4-morpholinocarbo                               nyl                                                    225 SCH.sub.3 phenyl 2-(aminosulfonyl)phenyl                                   226 SCH.sub.3 phenyl 2-(methylaminosulfonyl)phenyl                             227 SCH.sub.3 phenyl 1-pyrrolidinocarbonyl                                     228 SCH.sub.3 phenyl 2-(methylsulfonyl)phenyl                                  229 SCH.sub.3 phenyl 4-morpholino                                              230 SCH.sub.3 phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                      231 SCH.sub.3 phenyl 4-morpholinocarbonyl                                      232 SCH.sub.3 2-pyridyl 2-(aminosulfonyl)phenyl                                233 SCH.sub.3 2-pyridyl 2-(methylaminosulfonyl)phenyl                          234 SCH.sub.3 2-pyridyl 1-pyrrolidinocarbonyl                                  235 SCH.sub.3 2-pyridyl 2-(methylsulfonyl)phenyl                               236 SCH.sub.3 2-pyridyl 4-morpholino                                           237 SCH.sub.3 2-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                   238 SCH.sub.3 2-pyridyl 4-morpholinocarbonyl                                   239 SCH.sub.3 3-pyridyl 2-(aminosulfonyl)phenyl                                240 SCH.sub.3 3-pyridyl 2-(methylaminosulfonyl)phenyl                          241 SCH.sub.3 3-pyridyl 1-pyrrolidinocarbonyl                                  242 SCH.sub.3 3-pyridyl 2-(methylsulfonyl)phenyl                               243 SCH.sub.3 3-pyridyl 4-morpholino                                           244 SCH.sub.3 3-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                   245 SCH.sub.3 3-pyridyl 4-morpholinocarbonyl                                   246 SCH.sub.3 2-pyrimidyl 2-(aminosulfonyl)phenyl                              247 SCH.sub.3 2-pyrimidyl 2-(methylaminosulfonyl)phenyl                        248 SCH.sub.3 2-pyrimidyl 1-pyrrolidinocarbonyl                                249 SCH.sub.3 2-pyrimidyl 2-(methylsulfonyl)phenyl                             250 SCH.sub.3 2-pyrimidyl 4-morpholino                                         251 SCH.sub.3 2-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                 252 SCH.sub.3 2-pyrimidyl 4-morpholinocarbonyl                                 253 SCH.sub.3 5-pyrimidyl 2-(aminosulfonyl)phenyl                              254 SCH.sub.3 5-pyrimidyl 2-(methylaminosulfonyl)phenyl                        255 SCH.sub.3 5-pyrimidyl 1-pyrrolidinocarbonyl                                256 SCH.sub.3 5-pyrimidyl 2-(methylsulfonyl)phenyl                             257 SCH.sub.3 5-pyrimidyl 4-morpholino                                         258 SCH.sub.3 5-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                 259 SCH.sub.3 5-pyrimidyl 4-morpholinocarbonyl                                 260 SCH.sub.3 2-Cl-phenyl 2-(aminosulfonyl)phenyl                              261 SCH.sub.3 2-Cl-phenyl 2-(methylaminosulfonyl)phenyl                        262 SCH.sub.3 2-Cl-phenyl 1-pyrrolidinocarbonyl                                263 SCH.sub.3 2-Cl-phenyl 2-(methylsulfonyl)phenyl                             264 SCH.sub.3 2-Cl-phenyl 4-morpholino                                         265 SCH.sub.3 2-Cl-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                 266 SCH.sub.3 2-Cl-phenyl 4-morpholinocarbonyl                                 267 SCH.sub.3 2-F-phenyl 2-(aminosulfonyl)phenyl                               268 SCH.sub.3 2-F-phenyl 2-(methylaminosulfonyl)phenyl                         269 SCH.sub.3 2-F-phenyl 1-pyrrolidinocarbonyl                                 270 SCH.sub.3 2-F-phenyl 2-(methylsulfonyl)phenyl                              271 SCH.sub.3 2-F-phenyl 4-morpholino                                          272 SCH.sub.3 2-F-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                  273 SCH.sub.3 2-F-phenyl 4-morpholinocarbonyl                                  274 SCH.sub.3 2,5-diF-phenyl 2-(aminosulfonyl)phenyl                           275 SCH.sub.3 2,5-diF-phenyl 2-(methylaminosulfonyl)phenyl                     276 SCH.sub.3 2,5-diF-phenyl 1-pyrrolidinocarbonyl                             277 SCH.sub.3 2,5-diF-phenyl 2-(methylsulfonyl)phenyl                          278 SCH.sub.3 2,5-diF-phenyl 4-morpholino                                      279 SCH.sub.3 2,5-diF-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                       280 SCH.sub.3 2,5-diF-phenyl 4-morpholinocarbon                               yl                                                     281 SO.sub.2 CH.sub.3 phenyl 2-(aminosulfonyl)phenyl                           282 SO.sub.2 CH.sub.3 phenyl 2-(methylaminosulfonyl)phenyl                     283 SO.sub.2 CH.sub.3 phenyl 1-pyrrolidinocarbonyl                             284 SO.sub.2 CH.sub.3 phenyl 2-(methylsulfonyl)phenyl                          285 SO.sub.2 CH.sub.3 phenyl 4-morpholino                                      286 SO.sub.2 CH.sub.3 phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                       287 SO.sub.2 CH.sub.3 phenyl 4-morpholinocarbon                               yl                                                     288 SO.sub.2 CH.sub.3 2-pyridyl 2-(aminosulfonyl)phenyl                        289 SO.sub.2 CH.sub.3 2-pyridyl 2-(methylaminosulfonyl)phenyl                  290 SO.sub.2 CH.sub.3 2-pyridyl 1-pyrrolidinocarbonyl                          291 SO.sub.2 CH.sub.3 2-pyridyl 2-(methylsulfonyl)phenyl                       292 SO.sub.2 CH.sub.3 2-pyridyl 4-morpholino                                   293 SO.sub.2 CH.sub.3 2-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                    294 SO.sub.2 CH.sub.3 2-pyridyl 4-morpholinocar                               bonyl                                                  295 SO.sub.2 CH.sub.3 3-pyridyl 2-(aminosulfonyl)phenyl                        296 SO.sub.2 CH.sub.3 3-pyridyl 2-(methylaminosulfonyl)phenyl                  297 SO.sub.2 CH.sub.3 3-pyridyl 1-pyrrolidinocarbonyl                          298 SO.sub.2 CH.sub.3 3-pyridyl 2-(methylsulfonyl)phenyl                       299 SO.sub.2 CH.sub.3 3-pyridyl 4-morpholino                                   300 SO.sub.2 CH.sub.3 3-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                    301 SO.sub.2 CH.sub.3 3-pyridyl 4-morpholinocar                               bonyl                                                  302 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(aminosulfonyl)phenyl                      303 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(methylaminosulfonyl)phenyl                                         304 SO.sub.2 CH.sub.3 2-pyrimidyl 1-pyrrolidino                               carbonyl                                               305 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(methylsulfonyl)phenyl                     306 SO.sub.2 CH.sub.3 2-pyrimidyl 4-morpholino                                 307 SO.sub.2 CH.sub.3 2-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                  308 SO.sub.2 CH.sub.3 2-pyrimidyl 4-morpholinoc                               arbonyl                                                309 SO.sub.2 CH.sub.3 5-pyrimidyl 2-(aminosulfonyl)phenyl                      310 SO.sub.2 CH.sub.3 5-pyrimidyl 2-(methylaminosulfonyl)phenyl                                         311 SO.sub.2 CH.sub.3 5-pyrimidyl 1-pyrrolidino                               carbonyl                                               312 SO.sub.2 CH.sub.3 5-pyrimidyl 2-(methylsulfonyl)phenyl                     313 SO.sub.2 CH.sub.3 5-pyrimidyl 4-morpholino                                 314 SO.sub.2 CH.sub.3 5-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                  315 SO.sub.2 CH.sub.3 5-pyrimidyl 4-morpholinoc                               arbonyl                                                316 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(aminosulfonyl)phenyl                      317 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(methylaminosulfonyl)phenyl                                         318 SO.sub.2 CH.sub.3 2-Cl-phenyl 1-pyrrolidino                               carbonyl                                               319 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(methylsulfonyl)phenyl                     320 SO.sub.2 CH.sub.3 2-Cl-phenyl 4-morpholino                                 321 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                  322 SO.sub.2 CH.sub.3 2-Cl-phenyl 4-morpholinoc                               arbonyl                                                323 SO.sub.2 CH.sub.3 2-F-phenyl 2-(aminosulfonyl)phenyl                       324 SO.sub.2 CH.sub.3 2-F-phenyl 2-(methylaminosulfonyl)phenyl                 325 SO.sub.2 CH.sub.3 2-F-phenyl 1-pyrrolidinocarbonyl                         326 SO.sub.2 CH.sub.3 2-F-phenyl 2-(methylsulfonyl)phenyl                      327 SO.sub.2 CH.sub.3 2-F-phenyl 4-morpholino                                  328 SO.sub.2 CH.sub.3 2-F-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                   329 SO.sub.2 CH.sub.3 2-F-phenyl 4-morpholinoca                               rbonyl                                                 330 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(aminosulfonyl)phenyl                   331 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(methylaminosulfonyl)phenyl                                      332 SO.sub.2 CH.sub.3 2,5-diF-phenyl 1-pyrrolid                               inocarbonyl                                            333 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(methylsulfonyl)phenyl                  334 SO.sub.2 CH.sub.3 2,5-diF-phenyl 4-morpholino                              335 SO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)pheny                               l                                                      336 SO.sub.2 CH.sub.3 2,5-diF-phenyl 4-morpholinocarbonyl                      337 NHSO.sub.2 CH.sub.3 phenyl 2-(aminosulfonyl)phenyl                         338 NHSO.sub.2 CH.sub.3 phenyl 2-(methylaminosulfonyl)phenyl                   339 NHSO.sub.2 CH.sub.3 phenyl 1-pyrrolidinocarbonyl                           340 NHSO.sub.2 CH.sub.3 phenyl 2-(methylsulfonyl)phenyl                        341 NHSO.sub.2 CH.sub.3 phenyl 4-morpholino                                    342 NHSO.sub.2 CH.sub.3 phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                     343 NHSO.sub.2 CH.sub.3 phenyl 4-morpholinocarb                               onyl                                                   344 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(aminosulfonyl)phenyl                      345 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(methylaminosulfonyl)phenyl                                         346 NHSO.sub.2 CH.sub.3 2-pyridyl 1-pyrrolidino                               carbonyl                                               347 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(methylsulfonyl)phenyl                     348 NHSO.sub.2 CH.sub.3 2-pyridyl 4-morpholino                                 349 NHSO.sub.2 CH.sub.3 2-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                  350 NHSO.sub.2 CH.sub.3 2-pyridyl 4-morpholinoc                               arbonyl                                                351 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(aminosulfonyl)phenyl                      352 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(methylaminosulfonyl)phenyl                                         353 NHSO.sub.2 CH.sub.3 3-pyridyl 1-pyrrolidino                               carbonyl                                               354 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(methylsulfonyl)phenyl                     355 NHSO.sub.2 CH.sub.3 3-pyridyl 4-morpholino                                 356 NHSO.sub.2 CH.sub.3 3-pyridyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl                                  357 NHSO.sub.2 CH.sub.3 3-pyridyl 4-morpholinoc                               arbonyl                                                358 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(aminosulfonyl)phenyl                    359 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(methylaminosulfonyl)phenyl                                       360 NHSO.sub.2 CH.sub.3 2-pyrimidyl 1-pyrrolidi                               nocarbonyl                                             361 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(methylsulfonyl)phenyl                   362 NHSO.sub.2 CH.sub.3 2-pyrimidyl 4-morpholino                               363 NHSO.sub.2 CH.sub.3 2-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl       364 NHSO.sub.2 CH.sub.3 2-pyrimidyl 4-morpholinocarbonyl                       365 NHSO.sub.2 CH.sub.3 5-pyrimidyl 2-(aminosulfonyl)phenyl                    366 NHSO.sub.2 CH.sub.3 5-pyrimidyl 2-(methylaminosulfonyl)phenyl                                       367 NHSO.sub.2 CH.sub.3 5-pyrimidyl 1-pyrrolidi                               nocarbonyl                                             368 NHSO.sub.2 CH.sub.3 5-pyrimidyl 2-(methylsulfonyl)phenyl                   369 NHSO.sub.2 CH.sub.3 5-pyrimidyl 4-morpholino                               370 NHSO.sub.2 CH.sub.3 5-pyrimidyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl       371 NHSO.sub.2 CH.sub.3 5-pyrimidyl 4-morpholinocarbonyl                       372 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(aminosulfonyl)phenyl                    373 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(methylaminosulfonyl)phenyl                                       374 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 1-pyrrolidi                               nocarbonyl                                             375 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(methylsulfonyl)phenyl                   376 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 4-morpholino                               377 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl       378 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 4-morpholinocarbonyl                       379 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(aminosulfonyl)phenyl                     380 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(methylaminosulfonyl)phenyl                                        381 NHSO.sub.2 CH.sub.3 2-F-phenyl 1-pyrrolidin                               ocarbonyl                                              382 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(methylsulfonyl)phenyl                    383 NHSO.sub.2 CH.sub.3 2-F-phenyl 4-morpholino                                384 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phenyl        385 NHSO.sub.2 CH.sub.3 2-F-phenyl 4-morpholinocarbonyl                        386 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(aminosulfonyl)phenyl                 387 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(methylaminosulfonyl)phenyl                                    388 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl                                        1-pyrrolidinocarbonyl                                  389 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(methylsulfonyl)phenyl                                         390 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl                                        4-morpholino                                           391 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 2-(1'-CF.sub.3 -tetrazol-2-yl)phe                               nyl                                                    392 NHSO.sub.2 CH.sub.3 2,5-diF-phenyl 4-morpholinocarbonyl                  ______________________________________                                    

                                      TABLE 5                                      __________________________________________________________________________      ##STR166##                                                                    __________________________________________________________________________                                                 #STR167##                                                                      #STR168##                                                                      #STR169##                          a.sub.1                                                                           R = F, D = NH.sub.2                                                                              b.sub.1                                                                           R = F, D = NH.sub.2                                                                              c.sub.1                                                                           R = F, D = NH.sub.2               __________________________________________________________________________       a.sub.2 R = H, D = NH.sub.2 b.sub.2 R = H, D = NH.sub.2 c.sub.2 R = H,                                                    D = NH.sub.2                        a.sub.3 R = F, D = CH.sub.2 NH.sub.2 b.sub.3 R = F, D = CH.sub.2                                                          NH.sub.2 c.sub.3 R = F, D =                                                    CH.sub.2 NH.sub.2                   a.sub.4 R = H, D = CH.sub.2 NH.sub.2 b.sub.4 R = H, D = CH.sub.2                                                          NH.sub.2 c.sub.4 R = H, D =                                                    CH.sub.2 NH.sub.2                   a.sub.5 R = F, D = C(═NH)NH.sub.2 b.sub.5 R = F, D = C(═NH)NH.su                                                  b.2 c.sub.5 R = F, D =                                                         C(═NH)NH.sub.2                  a.sub.6 R = H, D = C(═NH)NH.sub.2 b.sub.6 R = H, D = C(═NH)NH.su                                                  b.2 c.sub.6 R = H, D =                                                         C(═NH)NH.sub.2                  a.sub.7 R = F, D = C(O)NH.sub.2 b.sub.7 R = F, D = C(O)NH.sub.2 c.sub.7                                                   R = F, D = C(O)NH.sub.2                                                         a.sub.8 R = H, D = C(O)NH.su                                                  b.2 b.sub.8 R = H, D =                                                         C(O)NH.sub.2 c.sub.8 R = H,                                                    D = C(O)NH.sub.2                  __________________________________________________________________________                                                 #STR170##                                                                      #STR171##                                                                      #STR172##                          d.sub.1                                                                           R = F, D = NH.sub.2                                                                              e.sub.1                                                                           R = F, D = NH.sub.2                                                                              f.sub.1                                                                           R = F, D = NH.sub.2               __________________________________________________________________________       d.sub.2 R = H, D = NH.sub.2 e.sub.2 R = H, D = NH.sub.2 f.sub.2 R = H,                                                    D = NH.sub.2                        d.sub.3 R = F, D = CH.sub.2 NH.sub.2 e.sub.3 R = F, D = CH.sub.2                                                          NH.sub.2 f.sub.3 R = F, D =                                                    CH.sub.2 NH.sub.2                   d.sub.4 R = H, D = CH.sub.2 NH.sub.2 e.sub.4 R = H, D = CH.sub.2                                                          NH.sub.2 f.sub.4 R = H, D =                                                    CH.sub.2 NH.sub.2                   d.sub.5 R = F, D = C(═NH)NH.sub.2 e.sub.5 R = F, D = C(═NH)NH.su                                                  b.2 f.sub.5 R = F, D =                                                         C(═NH)NH.sub.2                  d.sub.6 R = H, D = C(═NH)NH.sub.2 e.sub.6 R = H, D = C(═NH)NH.su                                                  b.2 f.sub.6 R = H, D =                                                         C(═NH)NH.sub.2                  d.sub.7 R = F, D = C(O)NH.sub.2 e.sub.7 R = F, D = C(O)NH.sub.2 f.sub.7                                                   R = F, D = C(O)NH.sub.2                                                         d.sub.8 R = H, D = C(O)NH.su                                                  b.2 e.sub.8 R = H, D =                                                         C(O)NH.sub.2 f.sub.8 R = H,                                                    D = C(O)NH.sub.2                  __________________________________________________________________________                                                 #STR173##                                                                      #STR174##                                                                      #STR175##                          g.sub.1                                                                           R = F, D = NH.sub.2                                                                              h.sub.1                                                                           R = F, D = NH.sub.2                                                                              i.sub.1                                                                           R = F, D = NH.sub.2               __________________________________________________________________________       g.sub.2 R = H, D = NH.sub.2 h.sub.2 R = H, D = NH.sub.2 i.sub.2 R = H,                                                    D = NH.sub.2                        g.sub.3 R = F, D = CH.sub.2 NH.sub.2 h.sub.3 R = F, D = CH.sub.2                                                          NH.sub.2 i.sub.3 R = F, D =                                                    CH.sub.2 NH.sub.2                   g.sub.4 R = H, D = CH.sub.2 NH.sub.2 h.sub.4 R = H, D = CH.sub.2                                                          NH.sub.2 i.sub.4 R = H, D =                                                    CH.sub.2 NH.sub.2                   g.sub.5 R = F, D = C(═NH)NH.sub.2 h.sub.5 R = F, D = C(═NH)NH.su                                                  b.2 i.sub.5 R = F, D =                                                         C(═NH)NH.sub.2                  g.sub.6 R = H, D = C(═NH)NH.sub.2 h.sub.6 R = H, D = C(═NH)NH.su                                                  b.2 i.sub.6 R = H, D =                                                         C(═NH)NH.sub.2                  g.sub.7 R = F, D = C(O)NH.sub.2 h.sub.7 R = F, D = C(O)NH.sub.2 i.sub.7                                                   R = F, D = C(O)NH.sub.2                                                         g.sub.8 R = H, D = C(O)NH.su                                                  b.2 h.sub.8 R = H, D =                                                         C(O)NH.sub.2 i.sub.8 R = H,                                                    D = C(O)NH.sub.2                  __________________________________________________________________________                                                 #STR176##                                                                      #STR177##                                                                      #STR178##                          j.sub.1                                                                           R = F, D = NH.sub.2                                                                              k.sub.1                                                                           R = F, D = NH.sub.2                                                                              l.sub.1                                                                           R = F, D = NH.sub.2               __________________________________________________________________________       j.sub.2 R = H, D = NH.sub.2 k.sub.2 R = H, D = NH.sub.2 l.sub.2 R = H,                                                    D = NH.sub.2                        j.sub.3 R = F, D = CH.sub.2 NH.sub.2 k.sub.3 R = F, D = CH.sub.2                                                          NH.sub.2 l.sub.3 R = F, D =                                                    CH.sub.2 NH.sub.2                   j.sub.4 R = H, D = CH.sub.2 NH.sub.2 k.sub.4 R = H, D = CH.sub.2                                                          NH.sub.2 l.sub.4 R = H, D =                                                    CH.sub.2 NH.sub.2                   j.sub.5 R = F, D = C(═NH)NH.sub.2 k.sub.5 R = F, D = C(═NH)NH.su                                                  b.2 l.sub.5 R = F, D =                                                         C(═NH)NH.sub.2                  j.sub.6 R = H, D = C(═NH)NH.sub.2 k.sub.6 R = H, D = C(═NH)NH.su                                                  b.2 l.sub.6 R = H, D =                                                         C(═NH)NH.sub.2                  j.sub.7 R = F, D = C(O)NH.sub.2 k.sub.7 R = F, D = C(O)NH.sub.2 l.sub.7                                                   R = F, D = C(O)NH.sub.2                                                         j.sub.8 R = H, D = C(O)NH.su                                                  b.2 k.sub.8 R = H, D =                                                         C(O)NH.sub.2 l.sub.8 R = H,                                                    D = C(O)NH.sub.2                  __________________________________________________________________________                                                 #STR179##                                                                      #STR180##                                                                      #STR181##                          m.sub.1                                                                           R = F, D = NH.sub.2                                                                              n.sub.1                                                                           R = F, D = NH.sub.2                                                                              o.sub.1                                                                           R = F, D = NH.sub.2               __________________________________________________________________________       m.sub.2 R = H, D = NH.sub.2 n.sub.2 R = H, D = NH.sub.2 o.sub.2 R = H,                                                    D = NH.sub.2                        m.sub.3 R = F, D = CH.sub.2 NH.sub.2 n.sub.3 R = F, D = CH.sub.2                                                          NH.sub.2 o.sub.3 R = F, D =                                                    CH.sub.2 NH.sub.2                   m.sub.4 R = H, D = CH.sub.2 NH.sub.2 n.sub.4 R = H, D = CH.sub.2                                                          NH.sub.2 o.sub.4 R = H, D =                                                    CH.sub.2 NH.sub.2                   m.sub.5 R = F, D = C(═NH)NH.sub.2 n.sub.5 R = F, D = C(═NH)NH.su                                                  b.2 o.sub.5 R = F, D =                                                         C(═NH)NH.sub.2                  m.sub.6 R = H, D = C(═NH)NH.sub.2 n.sub.6 R = H, D = C(═NH)NH.su                                                  b.2 o.sub.6 R = H, D =                                                         C(═NH)NH.sub.2                  m.sub.7 R = F, D = C(O)NH.sub.2 n.sub.7 R = F, D = C(O)NH.sub.2 o.sub.7                                                   R = F, D = C(O)NH.sub.2                                                         m.sub.8 R = H, D = C(O)NH.su                                                  b.2 n.sub.8 R = H, D =                                                         C(O)NH.sub.2 o.sub.8 R = H,                                                    D = C(O)NH.sub.2                  __________________________________________________________________________                                                 #STR182##                                                                      #STR183##                                                                      #STR184##                          p.sub.1                                                                           R = F, D = NH.sub.2                                                                              q.sub.1                                                                           R = F, D = NH.sub.2                                                                              r.sub.1                                                                           R = F, D = NH.sub.2               __________________________________________________________________________       p.sub.2 R = Cl, D = NH.sub.2 q.sub.2 R = Cl, D = NH.sub.2 r.sub.2 R =                                                     Cl, D = NH.sub.2                    p.sub.3 R = OMe, D = NH.sub.2 q.sub.3 R = OMe, D = NH.sub.2 r.sub.3 R =                                                   OMe, D = NH.sub.2                   p.sub.4 R = F, D = CH.sub.2 NH.sub.2 q.sub.4 R = F, D = CH.sub.2                                                          NH.sub.2 r.sub.4 R = F, D =                                                    CH.sub.2 NH.sub.2                   p.sub.5 R = Cl, D = CH.sub.2 NH.sub.2 q.sub.5 R = Cl, D = CH.sub.2                                                        NH.sub.2 r.sub.5 R = Cl, D =                                                   CH.sub.2 NH.sub.2                   p.sub.6 R = OMe, D = CH.sub.2 NH.sub.2 q.sub.6 R = OMe, D = CH.sub.2                                                      NH.sub.2 r.sub.6 R = OMe, D                                                    = CH.sub.2 NH.sub.2                 p.sub.7 R = F, D = C(═NH)NH.sub.2 q.sub.7 R = F, D = C(═NH)NH.su                                                  b.2 r.sub.7 R = F, D =                                                         C(═NH)NH.sub.2                  p.sub.8 R = Cl, D = C(═NH)NH.sub.2 q.sub.8 R = Cl, D = C(═NH)NH.                                                  sub.2 r.sub.8 R = Cl, D =                                                      C(═NH)NH.sub.2                  p.sub.9 R = OMe, D = C(═NH)NH.sub.2 q.sub.9 R = OMe, D = C(═NH)N                                                  H.sub.2 r.sub.9 R = OMe, D =                                                   C(═NH)NH.sub.2                  p.sub.10 R = F, D = C(O)NH.sub.2 q.sub.10 R = F, D = C(O)NH.sub.2                                                         r.sub.10 R = F, D = C(O)NH.su                                                  b.2                                 p.sub.11 R = Cl, D = C(O)NH.sub.2 q.sub.11 R = Cl, D = C(O)NH.sub.2                                                       r.sub.11 R = Cl, D =                                                           C(O)NH.sub.2                        p.sub.12 R = OMe, D = C(O)NH.sub.2 q.sub.12 R = OMe, D = C(O)NH.sub.2                                                     r.sub.12 R = OMe, D =                                                          C(O)NH.sub.2                      __________________________________________________________________________                                                 #STR185##                                                                      #STR186##                                                                      #STR187##                          s.sub.1                                                                           R = F, D = NH.sub.2                                                                              t.sub.1                                                                           R = F, D = NH.sub.2                                                                              u.sub.1                                                                           R = F, D = NH.sub.2               __________________________________________________________________________       s.sub.2 R = Cl, D = NH.sub.2 t.sub.2 R = Cl, D = NH.sub.2 u.sub.2 R =                                                     Cl, D = NH.sub.2                    s.sub.3 R = OMe, D = NH.sub.2 t.sub.3 R = OMe, D = NH.sub.2 u.sub.3 R =                                                   OMe, D = NH.sub.2                   s.sub.4 R = F, D = CH.sub.2 NH.sub.2 t.sub.4 R = F, D = CH.sub.2                                                          NH.sub.2 u.sub.4 R = F, D =                                                    CH.sub.2 NH.sub.2                   s.sub.5 R = Cl, D = CH.sub.2 NH.sub.2 t.sub.5 R = Cl, D = CH.sub.2                                                        NH.sub.2 u.sub.5 R = Cl, D =                                                   CH.sub.2 NH.sub.2                   s.sub.6 R = OMe, D = CH.sub.2 NH.sub.2 t.sub.6 R = OMe, D = CH.sub.2                                                      NH.sub.2 u.sub.6 R = OMe, D                                                    = CH.sub.2 NH.sub.2                 s.sub.7 R = F, D = C(═NH)NH.sub.2 t.sub.7 R = F, D = C(═NH)NH.su                                                  b.2 u.sub.7 R = F, D =                                                         C(═NH)NH.sub.2                  s.sub.8 R = Cl, D = C(═NH)NH.sub.2 t.sub.8 R = Cl, D = C(═NH)NH.                                                  sub.2 u.sub.8 R = Cl, D =                                                      C(═NH)NH.sub.2                  s.sub.9 R = OMe, D = C(═NH)NH.sub.2 t.sub.9 R = OMe, D = C(═NH)N                                                  H.sub.2 u.sub.9 R = OMe, D =                                                   C(═NH)NH.sub.2                  s.sub.10 R = F, D = C(O)NH.sub.2 t.sub.10 R = F, D = C(O)NH.sub.2                                                         u.sub.10 R = F, D = C(O)NH.su                                                  b.2                                 s.sub.11 R = Cl, D = C(O)NH.sub.2 t.sub.11 R = Cl, D = C(O)NH.sub.2                                                       u.sub.11 R = Cl, D =                                                           C(O)NH.sub.2                        s.sub.12 R = OMe, D = C(O)NH.sub.2 t.sub.12 R = OMe, D = C(O)NH.sub.2                                                     u.sub.12 R = OMe, D =                                                          C(O)NH.sub.2                      __________________________________________________________________________                                                 #STR188##                                                                      #STR189##                                                                      #STR190##                          v.sub.1                                                                           R = F, D = NH.sub.2                                                                              w.sub.1                                                                           R = F, D = NH.sub.2                                                                              x.sub.1                                                                           R = F, D = NH.sub.2               __________________________________________________________________________       v.sub.2 R = Cl, D = NH.sub.2 w.sub.2 R = Cl, D = NH.sub.2 x.sub.2 R =                                                     Cl, D = NH.sub.2                    v.sub.3 R = OMe, D = NH.sub.2 w.sub.3 R = OMe, D = NH.sub.2 x.sub.3 R =                                                   OMe, D = NH.sub.2                   v.sub.4 R = F, D = CH.sub.2 NH.sub.2 w.sub.4 R = F, D = CH.sub.2                                                          NH.sub.2 x.sub.4 R = F, D =                                                    CH.sub.2 NH.sub.2                   v.sub.5 R = Cl, D = CH.sub.2 NH.sub.2 w.sub.5 R = Cl, D = CH.sub.2                                                        NH.sub.2 x.sub.5 R = Cl, D =                                                   CH.sub.2 NH.sub.2                   v.sub.6 R = OMe, D = CH.sub.2 NH.sub.2 w.sub.6 R = OMe, D = CH.sub.2                                                      NH.sub.2 x.sub.6 R = OMe, D                                                    = CH.sub.2 NH.sub.2                 v.sub.7 R = F, D = C(═NH)NH.sub.2 w.sub.7 R = F, D = C(═NH)NH.su                                                  b.2 x.sub.7 R = F, D =                                                         C(═NH)NH.sub.2                  v.sub.8 R = Cl, D = C(═NH)NH.sub.2 w.sub.8 R = Cl, D = C(═NH)NH.                                                  sub.2 x.sub.8 R = Cl, D =                                                      C(═NH)NH.sub.2                  v.sub.9 R = OMe, D = C(═NH)NH.sub.2 w.sub.9 R = OMe, D = C(═NH)N                                                  H.sub.2 x.sub.9 R = OMe, D =                                                   C(═NH)NH.sub.2                  v.sub.10 R = F, D = C(O)NH.sub.2 w.sub.10 R = F, D = C(O)NH.sub.2                                                         x.sub.10 R = F, D = C(O)NH.su                                                  b.2                                 v.sub.11 R = Cl, D = C(O)NH.sub.2 w.sub.11 R = Cl, D = C(O)NH.sub.2                                                       x.sub.11 R = Cl, D =                                                           C(O)NH.sub.2                        v.sub.12 R = OMe, D = C(O)NH.sub.2 w.sub.12 R = OMe, D = C(O)NH.sub.2                                                     x.sub.12 R = OMe, D =                                                          C(O)NH.sub.2                      __________________________________________________________________________                                                 #STR191##                                                                      #STR192##                                                                      #STR193##                          y.sub.1                                                                           R = F, D = NH.sub.2                                                                              z.sub.1                                                                           R = F, D = NH.sub.2                                                                              aa.sub.1                                                                          R = F, D = NH.sub.2               __________________________________________________________________________       y.sub.2 R = Cl, D = NH.sub.2 z.sub.2 R = Cl, D = NH.sub.2 aa.sub.2 R =                                                    Cl, D = NH.sub.2                    y.sub.3 R = OMe, D = NH.sub.2 z.sub.3 R = OMe, D = NH.sub.2 aa.sub.3 R                                                    = OMe, D = NH.sub.2                 y.sub.4 R = F, D = CH.sub.2 NH.sub.2 z.sub.4 R = F, D = CH.sub.2                                                          NH.sub.2 aa.sub.4 R = F, D =                                                   CH.sub.2 NH.sub.2                   y.sub.5 R = Cl, D = CH.sub.2 NH.sub.2 z.sub.5 R = Cl, D = CH.sub.2                                                        NH.sub.2 aa.sub.5 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 y.sub.6 R = OMe, D = CH.sub.2 NH.sub.2 z.sub.6 R = OMe, D = CH.sub.2                                                      NH.sub.2 aa.sub.6 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 y.sub.7 R = F, D = C(═NH)NH.sub.2 z.sub.7 R = F, D = C(═NH)NH.su                                                  b.2 aa.sub.7 R = F, D =                                                        C(═NH)NH.sub.2                  y.sub.8 R = Cl, D = C(═NH)NH.sub.2 z.sub.8 R = Cl, D = C(═NH)NH.                                                  sub.2 aa.sub.8 R = Cl, D =                                                     C(═NH)NH.sub.2                  y.sub.9 R = OMe, D = C(═NH)NH.sub.2 z.sub.9 R = OMe, D = C(═NH)N                                                  H.sub.2 aa.sub.9 R = OMe, D                                                    = C(═NH)NH.sub.2                                                            y.sub.10 R = F, D =                                                           C(O)NH.sub.2 z.sub.10 R = F,                                                   D = C(O)NH.sub.2 aa.sub.10 R                                                   = F, D = C(O)NH.sub.2                                                           y.sub.11 R = Cl, D =                                                          C(O)NH.sub.2 z.sub.11 R =                                                      Cl, D = C(O)NH.sub.2                                                           aa.sub.11 R = Cl, D =                                                          C(O)NH.sub.2                        y.sub.12 R = OMe, D = C(O)NH.sub.2 z.sub.12 R = OMe, D = C(O)NH.sub.2                                                     aa.sub.12 R = OMe, D =                                                         C(O)NH.sub.2                      __________________________________________________________________________                                                 #STR194##                                                                      #STR195##                                                                      #STR196##                          bb.sub.1                                                                          R = F, D = NH.sub.2                                                                              cc.sub.1                                                                          R = F, D = NH.sub.2                                                                              dd.sub.1                                                                          R = F, D = NH.sub.2               __________________________________________________________________________       bb.sub.2 R = Cl, D = NH.sub.2 cc.sub.2 R = Cl, D = NH.sub.2 dd.sub.2 R                                                    = Cl, D = NH.sub.2                  bb.sub.3 R = OMe, D = NH.sub.2 cc.sub.3 R = OMe, D = NH.sub.2 dd.sub.3                                                    R = OMe, D = NH.sub.2                                                           bb.sub.4 R = F, D =                                                           CH.sub.2 NH.sub.2 cc.sub.4 R                                                   = F, D = CH.sub.2 NH.sub.2                                                     dd.sub.4 R = F, D = CH.sub.2                                                   NH.sub.2                            bb.sub.5 R = Cl, D = CH.sub.2 NH.sub.2 cc.sub.5 R = Cl, D = CH.sub.2                                                      NH.sub.2 dd.sub.5 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 bb.sub.6 R = OMe, D = CH.sub.2 NH.sub.2 cc.sub.6 R = OMe, D = CH.sub.2                                                    NH.sub.2 dd.sub.6 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 bb.sub.7 R = F, D = C(═NH)NH.sub.2 cc.sub.7 R = F, D = C(═NH)NH.                                                  sub.2 dd.sub.7 R = F, D =                                                      C(═NH)NH.sub.2                  bb.sub.8 R = Cl, D = C(═NH)NH.sub.2 cc.sub.8 R = Cl, D = C(═NH)N                                                  H.sub.2 dd.sub.8 R = Cl, D =                                                   C(═NH)NH.sub.2                  bb.sub.9 R = OMe, D = C(═NH)NH.sub.2 cc.sub.9 R = OMe, D = C(═NH                                                  )NH.sub.2 dd.sub.9 R = OMe,                                                    D = C(═NH)NH.sub.2                                                          bb.sub.10 R = F, D =                                                          C(O)NH.sub.2 cc.sub.10 R =                                                     F, D = C(O)NH.sub.2 dd.sub.10                                                   R = F, D = C(O)NH.sub.2                                                        bb.sub.11 R = Cl, D =                                                         C(O)NH.sub.2 cc.sub.11 R =                                                     Cl, D = C(O)NH.sub.2                                                           dd.sub.11 R = Cl, D =                                                          C(O)NH.sub.2                        bb.sub.12 R = OMe, D = C(O)NH.sub.2 cc.sub.12 R = OMe, D = C(O)NH.sub.2                                                   dd.sub.12 R = OMe, D =                                                         C(O)NH.sub.2                      __________________________________________________________________________                                                 #STR197##                                                                      #STR198##                                                                      #STR199##                          ee.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     ff.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     gg.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2      __________________________________________________________________________       ee.sub.2 R = Cl, D = CH.sub.2 NH.sub.2 ff.sub.2 R = Cl, D = CH.sub.2                                                      NH.sub.2 gg.sub.2 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 ee.sub.3 R = OMe, D = CH.sub.2 NH.sub.2 ff.sub.3 R = OMe, D = CH.sub.2                                                    NH.sub.2 gg.sub.3 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 ee.sub.4 R = CH.sub.2 NH.sub.2, ff.sub.4 R = CH.sub.2 NH.sub.2,                                                           gg.sub.4 R = CH.sub.2                                                          NH.sub.2,                            D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2         __________________________________________________________________________                                                 #STR200##                                                                      #STR201##                                                                      #STR202##                          hh.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     ii.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     jj.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2      __________________________________________________________________________       hh.sub.2 R = Cl, D = CH.sub.2 NH.sub.2 ii.sub.2 R = Cl, D = CH.sub.2                                                      NH.sub.2 jj.sub.2 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 hh.sub.3 R = OMe, D = CH.sub.2 NH.sub.2 ii.sub.3 R = OMe, D = CH.sub.2                                                    NH.sub.2 jj.sub.3 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 hh.sub.4 R = CH.sub.2 NH.sub.2, ii.sub.4 R = CH.sub.2 NH.sub.2,                                                           jj.sub.4 R = CH.sub.2                                                          NH.sub.2,                            D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2         __________________________________________________________________________                                                 #STR203##                                                                      #STR204##                                                                      #STR205##                          kk.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     ll.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     mm.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2      __________________________________________________________________________       kk.sub.2 R = Cl, D = CH.sub.2 NH.sub.2 ll.sub.2 R = Cl, D = CH.sub.2                                                      NH.sub.2 mm.sub.2 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 kk.sub.3 R = OMe, D = CH.sub.2 NH.sub.2 ll.sub.3 R = OMe, D = CH.sub.2                                                    NH.sub.2 mm.sub.3 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 kk.sub.4 R = CH.sub.2 NH.sub.2, ll.sub.4 R = CH.sub.2 NH.sub.2,                                                           mm.sub.4 R = CH.sub.2                                                          NH.sub.2,                            D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2         __________________________________________________________________________                                                 #STR206##                                                                      #STR207##                                                                      #STR208##                          nn.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     oo.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     pp.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2      __________________________________________________________________________       nn.sub.2 R = Cl, D = CH.sub.2 NH.sub.2 oo.sub.2 R = Cl, D = CH.sub.2                                                      NH.sub.2 pp.sub.2 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 nn.sub.3 R = OMe, D = CH.sub.2 NH.sub.2 oo.sub.3 R = OMe, D = CH.sub.2                                                    NH.sub.2 pp.sub.3 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 nn.sub.4 R = CH.sub.2 NH.sub.2, oo.sub.4 R = CH.sub.2 NH.sub.2,                                                           pp.sub.4 R = CH.sub.2                                                          NH.sub.2,                            D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2         __________________________________________________________________________                                                 #STR209##                                                                      #STR210##                                                                      #STR211##                          qq.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     rr.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2                                                                     ss.sub.1                                                                          R = F, D = CH.sub.2 NH.sub.2      __________________________________________________________________________       qq.sub.2 R = Cl, D = CH.sub.2 NH.sub.2 rr.sub.2 R = Cl, D = CH.sub.2                                                      NH.sub.2 ss.sub.2 R = Cl, D                                                    = CH.sub.2 NH.sub.2                 qq.sub.3 R = OMe, D = CH.sub.2 NH.sub.2 rr.sub.3 R = OMe, D = CH.sub.2                                                    NH.sub.2 ss.sub.3 R = OMe, D                                                   = CH.sub.2 NH.sub.2                 qq.sub.4 R = CH.sub.2 NH.sub.2, rr.sub.4 R = CH.sub.2 NH.sub.2,                                                           ss.sub.4 R = CH.sub.2                                                          NH.sub.2,                            D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2  D = CH.sub.2 NH.sub.2         __________________________________________________________________________

    ______________________________________                                         Ex#  R.sup.1b  A           B                                                   ______________________________________                                         1    H         phenyl      2-((Me).sub.2 N-methyl)phenyl                         2 H phenyl 2-((Me)NH-methyl)phenyl                                             3 H phenyl 2-(H.sub.2 N-methyl)phenyl                                          4 H phenyl 2-HOCH.sub.2 -phenyl                                                5 H 2-F-phenyl 2-((Me).sub.2 N-methyl)phenyl                                   6 H 2-F-phenyl 2-((Me)NH-methyl)phenyl                                         7 H 2-F-phenyl 2-(H.sub.2 N-methyl)phenyl                                      8 H 2-F-phenyl 2-HOCH.sub.2 -phenyl                                            9 H phenyl 2-methylimidazol-1-yl                                               10 H phenyl 2-ethylimidazol-1-yl                                               11 H phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                               12 H phenyl 2-CH.sub.3 NHSO.sub.2 -imidazol-1-yl                               13 H phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                                14 H 2-F-phenyl 2-methylimidazol-1-yl                                          15 H 2-F-phenyl 2-ethylimidazol-1-yl                                           16 H 2-F-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                           17 H 2-F-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                             18 H 2-F-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                            19 H 2-Cl-phenyl 2-methylimidazol-1-yl                                         20 H 2-Cl-phenyl 2-ethylimidazol-1-yl                                          21 H 2-Cl-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                          22 H 2-Cl-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                            23 H 2-Cl-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                           24 H 2-(Me).sub.2 N-phenyl 2-methylimidazol-1-yl                               25 H 2-(Me).sub.2 N-phenyl 2-ethylimidazol-1-yl                                26 H 2-(Me).sub.2 N-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                                          27 H 2-(Me).sub.2 N-phenyl 2-CH.sub.3                                         SO.sub.2 -imidazol-1-yl                               28 H 2-(Me).sub.2 N-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                 29 H phenyl N-methylimidazol-2-yl                                              30 H phenyl 4-methylimidazol-5-yl                                              31 H phenyl 5-CF.sub.3 -pyrazol-1-yl                                           32 H 2-F-phenyl N-methylimidazol-2-yl                                          33 H 2-F-phenyl 4-methylimidazol-5-yl                                          34 H 2-F-phenyl 5-CF.sub.3 -pyrazol-1-yl                                       35 H phenyl guanidino                                                          36 H phenyl 2-thiazolin-2-ylamine                                              37 H phenyl N-methyl-2-imidazolin-2-yl                                         38 H phenyl N-methyl-1,4,5,6-                                                     tetrahydropyrimid-2-yl                                                      39 H phenyl N-methylimidazol-2-ylthiol                                         40 H phenyl t-butoxycarbonylamine                                              41 H phenyl (N-pyrrolidino)formylimino                                         42 H phenyl (N-pyrrolidino)formyl-N-                                              (methanesulfamoyl)imino                                                     43 H 2-F-phenyl guanidino                                                      44 H 2-F-phenyl 2-thiazolin-2-ylamine                                          45 H 2-F-phenyl N-methyl-2-imidazolin-2-yl                                     46 H 2-F-phenyl N-methyl-1,4,5,6-                                                 tetrahydropyrimid-2-yl                                                      47 H 2-F-phenyl N-methylimidazol-2-ylthio                                      48 H 2-F-phenyl t-butoxycarbonylamine                                          49 H 2-F-phenyl (N-pyrrolidino)formylimino                                     50 H 2-F-phenyl (N-pyrrolidino)formyl-N-                                          (methanesulfamoyl)imino                                                     51 H 2-CH.sub.3 O-phenyl (N-pyrrolidino)formylimino                            52 H 2-CH.sub.3 O-phenyl (N-pyrrolidino)formyl-N-                                 (methanesulfamoyl)imino                                                     53 --CN phenyl 2-((Me).sub.2 N-methyl)phenyl                                   54 --CN phenyl 2-((Me)NH-methyl)phenyl                                         55 --CN phenyl 2-(H.sub.2 N-methyl)phenyl                                      56 --CN phenyl 2-HOCH.sub.2 -phenyl                                            57 --CN 2-F-phenyl 2-((Me).sub.2 N-methyl)phenyl                               58 --CN 2-F-phenyl 2-((Me)NH-methyl)phenyl                                     59 --CN 2-F-phenyl 2-(H.sub.2 N-methyl)phenyl                                  60 --CN 2-F-phenyl 2-HOCH.sub.2 -phenyl                                        61 --CN phenyl 2-methylimidazol-1-yl                                           62 --CN phenyl 2-ethylimidazol-1-yl                                            63 --CN phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                            64 --CN phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                              65 --CN phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                             66 --CN 2-F-phenyl 2-methylimidazol-1-yl                                       67 --CN 2-F-phenyl 2-ethylimidazol-1-yl                                        68 --CN 2-F-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                        69 --CN 2-F-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                          70 --CN 2-F-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                         71 --CN 2-Cl-phenyl 2-methylimidazol-1-yl                                      72 --CN 2-Cl-phenyl 2-ethylimidazol-1-yl                                       73 --CN 2-Cl-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                       74 --CN 2-Cl-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                         75 --CN 2-Cl-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                        76 --CN 2-(Me).sub.2 N-phenyl 2-methylimidazol-1-yl                            77 --CN 2-(Me).sub.2 N-phenyl 2-ethylimidazol-1-yl                             78 --CN 2-(Me).sub.2 N-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                                       79 --CN 2-(Me).sub.2 N-phenyl 2-CH.sub.3                                      SO.sub.2 -imidazol-1-yl                               80 --CN 2-(Me).sub.2 N-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                                        81 --CN phenyl N-methylimidazol-2-yl                 82 --CN phenyl 4-methylimidazol-5-yl                                           83 --CN phenyl 5-CF.sub.3 -pyrazol-1-yl                                        84 --CN 2-F-phenyl N-methylimidazol-2-yl                                       85 --CN 2-F-phenyl 4-methylimidazol-5-yl                                       86 --CN 2-F-phenyl 5-CF.sub.3 -pyrazol-1-yl                                    87 --CN phenyl guanidino                                                       88 --CN phenyl 2-thiazolin-2-ylamine                                           89 --CN phenyl N-methyl-2-imidazolin-2-yl                                      90 --CN phenyl N-methyl-1,4,5,6-                                                  tetrahydropyrimid-2-yl                                                      91 --CN phenyl N-methylimidazol-2-ylthiol                                      92 --CN phenyl t-butoxycarbonylamine                                           93 --CN phenyl (N-pyrrolidino)formylimino                                      94 --CN phenyl (N-pyrrolidino)formyl-N-                                           (methanesulfamoyl)imino                                                     95 --CN 2-F-phenyl guanidino                                                   96 --CN 2-F-phenyl 2-thiazolin-2-ylamine                                       97 --CN 2-F-phenyl N-methyl-2-imidazolin-2-yl                                  98 --CN 2-F-phenyl N-methyl-1,4,5,6-                                              tetrahydropyrimid-2-yl                                                      99 --CN 2-F-phenyl N-methylimidazol-2-ylthio                                   100 --CN 2-F-phenyl t-butoxycarbonylamine                                      101 --CN 2-F-phenyl (N-pyrrolidino)formylimino                                 102 --CN 2-F-phenyl (N-pyrrolidino)formyl-N-                                      (methanesulfamoyl)imino                                                     103 --CN 2-CH.sub.3 O-phenyl (N-pyrrolidino)formylimino                        104 --CN 2-CH.sub.3 O-phenyl (N-pyrrolidino)formyl-N-                             (methanesulfamoyl)imino                                                     105 CF.sub.3  phenyl 2-((Me).sub.2 N-methyl)phenyl                             106 CF.sub.3  phenyl 2-((Me)NH-methyl)phenyl                                   107 CF.sub.3  phenyl 2-(H.sub.2 N-methyl)phenyl                                108 CF.sub.3  phenyl 2-HOCH.sub.2 -phenyl                                      109 CF.sub.3  2-F-phenyl 2-((Me).sub.2 N-methyl)phenyl                         110 CF.sub.3  2-F-phenyl 2-((Me)NH-methyl)phenyl                               111 CF.sub.3  2-F-phenyl 2-(H.sub.2 N-methyl)phenyl                            112 CF.sub.3  2-F-phenyl 2-HOCH.sub.2 -phenyl                                  113 CF.sub.3  phenyl 2-methylimidazol-1-yl                                     114 CF.sub.3  phenyl 2-ethylimidazol-1-yl                                      115 CF.sub.3  phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                      116 CF.sub.3  phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                        117 CF.sub.3  phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                       118 CF.sub.3  2-F-phenyl 2-methylimidazol-1-yl                                 119 CF.sub.3  2-F-phenyl 2-ethylimidazol-1-yl                                  120 CF.sub.3  2-F-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                  121 CF.sub.3  2-F-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                    122 CF.sub.3  2-F-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                   123 CF.sub.3  2-Cl-phenyl 2-methylimidazol-1-yl                                124 CF.sub.3  2-Cl-phenyl 2-ethylimidazol-1-yl                                 125 CF.sub.3  2-Cl-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                 126 CF.sub.3  2-Cl-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                   127 CF.sub.3  2-Cl-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                  128 CF.sub.3  2-(Me).sub.2 N-phenyl 2-methylimidazol-1-yl                      129 CF.sub.3  2-(Me).sub.2 N-phenyl 2-ethylimidazol-1-yl                       130 CF.sub.3  2-(Me).sub.2 N-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl       131 CF.sub.3  2-(Me).sub.2 N-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                                   132 CF.sub.3  2-(Me).sub.2 N-phenyl 2-CH.sub.3                                 OCH.sub.2 -imidazol-1-yl                             133 CF.sub.3  phenyl N-methylimidazol-2-yl                                     134 CF.sub.3  phenyl 4-methylimidazol-5-yl                                     135 CF.sub.3  phenyl 5-CF.sub.3 -pyrazol-1-yl                                  136 CF.sub.3  2-F-phenyl N-methylimidazol-2-yl                                 137 CF.sub.3  2-F-phenyl 4-methylimidazol-5-yl                                 138 CF.sub.3  2-F-phenyl 5-CF.sub.3 -pyrazol-1-yl                              139 CF.sub.3  phenyl guanidino                                                 140 CF.sub.3  phenyl 2-thiazolin-2-ylamine                                     141 CF.sub.3  phenyl N-methyl-2-imidazolin-2-yl                                142 CF.sub.3  phenyl N-methyl-1,4,5,6-                                            tetrahydropyrimid-2-yl                                                      143 CF.sub.3  phenyl N-methylimidazol-2-ylthiol                                144 CF.sub.3  phenyl t-butoxycarbonylamine                                     145 CF.sub.3  phenyl (N-pyrrolidino)formylimino                                146 CF.sub.3  phenyl (N-pyrrolidino)formyl-N-                                     (methanesulfamoyl)imino                                                     147 CF.sub.3  2-F-phenyl guanidino                                             148 CF.sub.3  2-F-phenyl 2-thiazolin-2-ylamine                                 149 CF.sub.3  2-F-phenyl N-methyl-2-imidazolin-2-yl                            150 CF.sub.3  2-F-phenyl N-methyl-1,4,5,6-                                        tetrahydropyrimid-2-yl                                                      151 CF.sub.3  2-F-phenyl N-methylimidazol-2-ylthio                             152 CF.sub.3  2-F-phenyl t-butoxycarbonylamine                                 153 CF.sub.3  2-F-phenyl (N-pyrrolidino)formylimino                            154 CF.sub.3  2-F-phenyl (N-pyrrolidino)formyl-N-                                 (methanesulfamoyl)imino                                                     155 CF.sub.3  2-CH.sub.3 O-phenyl (N-pyrrolidino)formylimino                   156 CF.sub.3  2-CH.sub.3 O-phenyl (N-pyrrolidino)formyl-N-                        (methanesulfamoyl)imino                                                     157 CONH.sub.2 phenyl 2-((Me).sub.2 N-methyl)phenyl                            158 CONH.sub.2 phenyl 2-((Me)NH-methyl)phenyl                                  159 CONH.sub.2 phenyl 2-(H.sub.2 N-methyl)phenyl                               160 CONH.sub.2 phenyl 2-HOCH.sub.2 -phenyl                                     161 CONH.sub.2 2-F-phenyl 2-((Me).sub.2 N-methyl)phenyl                        162 CONH.sub.2 2-F-phenyl 2-((Me)NH-methyl)phenyl                              163 CONH.sub.2 2-F-phenyl 2-(H.sub.2 N-methyl)phenyl                           164 CONH.sub.2 2-F-phenyl 2-HOCH.sub.2 -phenyl                                 165 CONH.sub.2 phenyl 2-methylimidazol-1-yl                                    166 CONH.sub.2 phenyl 2-ethylimidazol-1-yl                                     167 CONH.sub.2 phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                     168 CONH.sub.2 phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                       169 CONH.sub.2 phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                      170 CONH.sub.2 2-F-phenyl 2-methylimidazol-1-yl                                171 CONH.sub.2 2-F-phenyl 2-ethylimidazol-1-yl                                 172 CONH.sub.2 2-F-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                 173 CONH.sub.2 2-F-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                   174 CONH.sub.2 2-F-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-y1                  175 CONH.sub.2 2-Cl-phenyl 2-methylimidazol-1-yl                               176 CONH.sub.2 2-Cl-phenyl 2-ethylimidazol-1-yl                                177 CONH.sub.2 2-Cl-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                                          178 CONH.sub.2 2-Cl-phenyl 2-CH.sub.3                                         SO.sub.2 -imidazol-1-yl                               179 CONH.sub.2 2-Cl-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                 180 CONH.sub.2 2-(Me).sub.2 N-phenyl 2-methylimidazol-1-yl                     181 CONH.sub.2 2-(Me).sub.2 N-phenyl 2-ethylimidazol-1-yl                      182 CONH.sub.2 2-(Me).sub.2 N-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-y                                l                                                     183 CONH.sub.2 2-(Me).sub.2 N-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl        184 CONH.sub.2 2-(Me).sub.2 N-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl       185 CONH.sub.2 phenyl N-methylimidazol-2-yl                                    186 CONH.sub.2 phenyl 4-methylimidazol-5-yl                                    187 CONH.sub.2 phenyl 5-CF.sub.3 -pyrazol-1-yl                                 188 CONH.sub.2 2-F-phenyl N-methylimidazol-2-yl                                189 CONH.sub.2 2-F-phenyl 4-methylimidazol-5-yl                                190 CONH.sub.2 2-F-phenyl 5-CF.sub.3 -pyrazol-1-yl                             191 CONH.sub.2 phenyl guanidino                                                192 CONH.sub.2 phenyl 2-thiazolin-2-ylamine                                    193 CONH.sub.2 phenyl N-methyl-2-imidazolin-2-yl                               194 CONH.sub.2 phenyl N-methyl-1,4,5,6-                                           tetrahydropyrimid-2-yl                                                      195 CONH.sub.2 phenyl N-methylimidazol-2-ylthiol                               196 CONH.sub.2 phenyl t-butoxycarbonylamine                                    197 CONH.sub.2 phenyl (N-pyrrolidino)formylimino                               198 CONH.sub.2 phenyl (N-pyrrolidino)formyl-N-                                    (methanesulfamoyl)imino                                                     199 CONH.sub.2 2-F-phenyl guanidino                                            200 CONH.sub.2 2-F-phenyl 2-thiazolin-2-ylamine                                201 CONH.sub.2 2-F-phenyl N-methyl-2-imidazolin-2-yl                           202 CONH.sub.2 2-F-phenyl N-methyl-1,4,5,6-                                       tetrahydropyrimid-2-yl                                                      203 CONH.sub.2 2-F-phenyl N-methylimidazol-2-ylthio                            204 CONH.sub.2 2-F-phenyl t-butoxycarbonylamine                                205 CONH.sub.2 2-F-phenyl (N-pyrrolidino)formylimino                           206 CONH.sub.2 2-F-phenyl (N-pyrrolidino)formyl-N-                                (methanesulfamoyl)imino                                                     207 CONH.sub.2 2-CH.sub.3 O-phenyl (N-pyrrolidino)formylimino                  208 CONH.sub.2 2-CH.sub.3 O-phenyl (N-pyrrolidino)formyl-N-                       (methanesulfamoyl)imino                                                     209 SCH.sub.3 phenyl 2-((Me).sub.2 N-methyl)phenyl                             210 SCH.sub.3 phenyl 2-((Me)NH-methyl)phenyl                                   211 SCH.sub.3 phenyl 2-(H.sub.2 N-methyl)phenyl                                212 SCH.sub.3 phenyl 2-HOCH.sub.2 -phenyl                                      213 SCH.sub.3 2-F-phenyl 2-((Me).sub.2 N-methyl)phenyl                         214 SCH.sub.3 2-F-phenyl 2-((Me)NH-methyl)phenyl                               215 SCH.sub.3 2-F-phenyl 2-(H.sub.2 N-methyl)phenyl                            216 SCH.sub.3 2-F-phenyl 2-HOCH.sub.2 -phenyl                                  217 SCH.sub.3 phenyl 2-methylimidazol-1-yl                                     218 SCH.sub.3 phenyl 2-ethylimidazol-1-yl                                      219 SCH.sub.3 phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                      220 SCH.sub.3 phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                        221 SCH.sub.3 phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                       222 SCH.sub.3 2-F-phenyl 2-methylimidazol-1-yl                                 223 SCH.sub.3 2-F-phenyl 2-ethylimidazol-1-yl                                  224 SCH.sub.3 2-F-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                  225 SCH.sub.3 2-F-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                    226 SCH.sub.3 2-F-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                   227 SCH.sub.3 2-Cl-phenyl 2-methylimidazol-1-yl                                228 SCH.sub.3 2-Cl-phenyl 2-ethylimidazol-1-yl                                 229 SCH.sub.3 2-Cl-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                 230 SCH.sub.3 2-Cl-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                   231 SCH.sub.3 2-Cl-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                  232 SCH.sub.3 2-(Me).sub.2 N-phenyl 2-methylimidazol-1-yl                      233 SCH.sub.3 2-(Me).sub.2 N-phenyl 2-ethylimidazol-1-yl                       234 SCH.sub.3 2-(Me).sub.2 N-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl       235 SCH.sub.3 2-(Me).sub.2 N-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                                   236 SCH.sub.3 2-(Me).sub.2 N-phenyl 2-CH.sub.3                                 OCH.sub.2 -imidazol-1-yl                             237 SCH.sub.3 phenyl N-methylimidazol-2-yl                                     238 SCH.sub.3 phenyl 4-methylimidazol-5-yl                                     239 SCH.sub.3 phenyl 5-CF.sub.3 -pyrazol-1-yl                                  240 SCH.sub.3 2-F-phenyl N-methylimidazol-2-yl                                 241 SCH.sub.3 2-F-phenyl 4-methylimidazol-5-yl                                 242 SCH.sub.3 2-F-phenyl 5-CF.sub.3 -pyrazol-1-yl                              243 SCH.sub.3 phenyl guanidino                                                 244 SCH.sub.3 phenyl 2-thiazolin-2-ylamine                                     245 SCH.sub.3 phenyl N-methyl-2-imidazolin-2-yl                                246 SCH.sub.3 phenyl N-methyl-1,4,5,6-                                            tetrahydropyrimid-2-yl                                                      247 SCH.sub.3 phenyl N-methylimidazol-2-ylthiol                                248 SCH.sub.3 phenyl t-butoxycarbonylamine                                     249 SCH.sub.3 phenyl (N-pyrrolidino)formylimino                                250 SCH.sub.3 phenyl (N-pyrrolidino)formyl-N-                                     (methanesulfamoyl)imino                                                     251 SCH.sub.3 2-F-phenyl guanidino                                             252 SCH.sub.3 2-F-phenyl 2-thiazolin-2-ylamine                                 253 SCH.sub.3 2-F-phenyl N-methyl-2-imidazolin-2-yl                            254 SCH.sub.3 2-F-phenyl N-methyl-1,4,5,6-                                        tetrahydropyrimid-2-yl                                                      255 SCH.sub.3 2-F-phenyl N-methylimidazol-2-ylthio                             256 SCH.sub.3 2-F-phenyl t-butoxycarbonylamine                                 257 SCH.sub.3 2-F-phenyl (N-pyrrolidino)formylimino                            258 SCH.sub.3 2-F-phenyl (N-pyrrolidino)formyl-N-                                 (methanesulfamoyl)imino                                                     259 SCH.sub.3 2-CH.sub.3 O-phenyl (N-pyrrolidino)formylimino                   260 SCH.sub.3 2-CH.sub.3 O-phenyl (N-pyrrolidino)formyl-N-                        (methanesulfamoyl)imino                                                     261 SO.sub.2 CH.sub.3 phenyl 2-((Me).sub.2 N-methyl)phenyl                     262 SO.sub.2 CH.sub.3 phenyl 2-((Me)NH-methyl)phenyl                           263 SO.sub.2 CH.sub.3 phenyl 2-(H.sub.2 N-methyl)phenyl                        264 SO.sub.2 CH.sub.3 phenyl 2-HOCH.sub.2 -phenyl                              265 SO.sub.2 CH.sub.3 2-F-phenyl 2-((Me).sub.2 N-methyl)phenyl                 266 SO.sub.2 CH.sub.3 2-F-phenyl 2-((Me)NH-methyl)phenyl                       267 SO.sub.2 CH.sub.3 2-F-phenyl 2-(H.sub.2 N-methyl)phenyl                    268 SO.sub.2 CH.sub.3 2-F-phenyl 2-HOCH.sub.2 -phenyl                          269 SO.sub.2 CH.sub.3 phenyl 2-methylimidazol-1-yl                             270 SO.sub.2 CH.sub.3 phenyl 2-ethylimidazol-1-yl                              271 SO.sub.2 CH.sub.3 phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                                        272 SO.sub.2 CH.sub.3 phenyl 2-CH.sub.3                                       SO.sub.2 -imidazol-1-yl                               273 SO.sub.2 CH.sub.3 phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                                         274 SO.sub.2 CH.sub.3 2-F-phenyl 2-methylimida                                zol-1-yl                                              275 SO.sub.2 CH.sub.3 2-F-phenyl 2-ethylimidazol-1-yl                          276 SO.sub.2 CH.sub.3 2-F-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                                    277 SO.sub.2 CH.sub.3 2-F-phenyl 2-CH.sub.3                                   SO.sub.2 -imidazol-1-yl                               278 SO.sub.2 CH.sub.3 2-F-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                                     279 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-methylimid                                azol-1-yl                                             280 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-ethylimidazol-1-yl                         281 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                                   282 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-CH.sub.3                                  SO.sub.2 -imidazol-1-yl                               283 SO.sub.2 CH.sub.3 2-Cl-phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                                    284 SO.sub.2 CH.sub.3 2-(Me).sub.2 N-phenyl                                   2-methylimidazol-1-yl                                 285 SO.sub.2 CH.sub.3 2-(Me).sub.2 N-phenyl 2-ethylimidazol-1-yl                                         286 SO.sub.2 CH.sub.3 2-(Me).sub.2 N-phenyl                                   2-((Me).sub.2 N-methyl)imidazol-1-yl                  287 SO.sub.2 CH.sub.3 2-(Me).sub.2 N-phenyl 2-CH.sub.3 SO.sub.2                                         -imidazol-1-yl                                        288 SO.sub.2 CH.sub.3 2-(Me).sub.2 N-phenyl 2-CH.sub.3 OCH.sub.2                                        -imidazol-1-yl                                        289 SO.sub.2 CH.sub.3 phenyl N-methylimidazol-2-yl                             290 SO.sub.2 CH.sub.3 phenyl 4-methylimidazol-5-yl                             291 SO.sub.2 CH.sub.3 phenyl 5-CF.sub.3 -pyrazol-1-yl                          292 SO.sub.2 CH.sub.3 2-F-phenyl N-methylimidazol-2-yl                         293 SO.sub.2 CH.sub.3 2-F-phenyl 4-methylimidazol-5-yl                         294 SO.sub.2 CH.sub.3 2-F-phenyl 5-CF.sub.3 -pyrazol-1-yl                      295 SO.sub.2 CH.sub.3 phenyl guanidino                                         296 SO.sub.2 CH.sub.3 phenyl 2-thiazolin-2-ylamine                             297 SO.sub.2 CH.sub.3 phenyl N-methyl-2-imidazolin-2-yl                        298 SO.sub.2 CH.sub.3 phenyl N-methyl-1,4,5,6-                                    tetrahydropyrimid-2-yl                                                      299 SO.sub.2 CH.sub.3 phenyl N-methylimidazol-2-ylthiol                        300 SO.sub.2 CH.sub.3 phenyl t-butoxycarbonylamine                             301 SO.sub.2 CH.sub.3 phenyl (N-pyrrolidino)formylimino                        302 SO.sub.2 CH.sub.3 phenyl (N-pyrrolidino)formyl-N-                             (methanesulfamoyl)imino                                                     303 SO.sub.2 CH.sub.3 2-F-phenyl guanidino                                     304 SO.sub.2 CH.sub.3 2-F-phenyl 2-thiazolin-2-ylamine                         305 SO.sub.2 CH.sub.3 2-F-phenyl N-methyl-2-imidazolin-2-yl                    306 SO.sub.2 CH.sub.3 2-F-phenyl N-methyl-1,4,5,6-                                tetrahydropyrimid-2-yl                                                      307 SO.sub.2 CH.sub.3 2-F-phenyl N-methylimidazol-2-ylthio                     308 SO.sub.2 CH.sub.3 2-F-phenyl t-butoxycarbonylamine                         309 SO.sub.2 CH.sub.3 2-F-phenyl (N-pyrrolidino)formylimino                    310 SO.sub.2 CH.sub.3 2-F-phenyl (N-pyrrolidino)formyl-N-                         (methanesulfamoyl)imino                                                     311 SO.sub.2 CH.sub.3 2-CH.sub.3 O-phenyl (N-pyrrolidino)formylimino                                     312 SO.sub.2 CH.sub.3 2-CH.sub.3 O-phenyl                                     (N-pyrrolidino)formyl-N-                                 (methanesulfamoyl)imino                                                     313 NHSO.sub.2 CH.sub.3 phenyl 2-((Me).sub.2 N-methyl)phenyl                   314 NHSO.sub.2 CH.sub.3 phenyl 2-((Me)NH-methyl)phenyl                         315 NHSO.sub.2 CH.sub.3 phenyl 2-(H.sub.2 N-methyl)phenyl                      316 NHSO.sub.2 CH.sub.3 phenyl 2-HOCH.sub.2 -phenyl                            317 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-((Me).sub.2 N-methyl)phenyl                                         318 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-((Me)NH-m                                ethyl)phenyl                                          319 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-(H.sub.2 N-methyl)phenyl                  320 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-HOCH.sub.2 -phenyl                        321 NHSO.sub.2 CH.sub.3 phenyl 2-methylimidazol-1-yl                           322 NHSO.sub.2 CH.sub.3 phenyl 2-ethylimidazol-1-yl                            323 NHSO.sub.2 CH.sub.3 phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl                                      324 NHSO.sub.2 CH.sub.3 phenyl 2-CH.sub.3                                     SO.sub.2 -imidazol-1-yl                               325 NHSO.sub.2 CH.sub.3 phenyl 2-CH.sub.3 OCH.sub.2 -imidazol-1-yl                                       326 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-methylimi                                dazol-1-yl                                            327 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-ethylimidazol-1-yl                        328 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl        329 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                                    330 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-CH.sub.3                                 OCH.sub.2 -imidazol-1-yl                              331 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-methylimidazol-1-yl                      332 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-ethylimidazol-1-yl                       333 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-((Me).sub.2 N-methyl)imidazol-1-yl       334 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-CH.sub.3 SO.sub.2 -imidazol-1-yl                                   335 NHSO.sub.2 CH.sub.3 2-Cl-phenyl 2-CH.sub.3                                 OCH.sub.2 -imidazol-1-yl                             336 NHSO.sub.2 CH.sub.3 2-(Me).sub.2 N-phenyl 2-methylimidazol-1-yl                                      337 NHSO.sub.2 CH.sub.3 2-(Me).sub.2 N-phenyl                                 2-ethylimidazol-1-yl                                  338 NHSO.sub.2 CH.sub.3 2-(Me).sub.2 N-phenyl 2-((Me).sub.2 N-methyl)imi                                dazol-1-yl                                            339 NHSO.sub.2 CH.sub.3 2-(Me).sub.2 N-phenyl 2-CH.sub.3 SO.sub.2                                       -imidazol-1-yl                                        340 NHSO.sub.2 CH.sub.3 2-(Me).sub.2 N-phenyl 2-CH.sub.3 OCH.sub.2                                      -imidazol-1-yl                                        341 NHSO.sub.2 CH.sub.3 phenyl N-methylimidazol-2-yl                           342 NHSO.sub.2 CH.sub.3 phenyl 4-methylimidazol-5-yl                           343 NHSO.sub.2 CH.sub.3 phenyl 5-CF.sub.3 -pyrazol-1-yl                        344 NHSO.sub.2 CH.sub.3 2-F-phenyl N-methylimidazol-2-yl                       345 NHSO.sub.2 CH.sub.3 2-F-phenyl 4-methylimidazol-5-yl                       346 NHSO.sub.2 CH.sub.3 2-F-phenyl 5-CF.sub.3 -pyrazol-1-yl                    347 NHSO.sub.2 CH.sub.3 phenyl guanidino                                       348 NHSO.sub.2 CH.sub.3 phenyl 2-thiazolin-2-ylamine                           349 NHSO.sub.2 CH.sub.3 phenyl N-methyl-2-imidazolin-2-yl                      350 NHSO.sub.2 CH.sub.3 phenyl N-methyl-1,4,5,6-                                  tetrahydropyrimid-2-yl                                                      351 NHSO.sub.2 CH.sub.3 phenyl N-methylimidazol-2-ylthiol                      352 NHSO.sub.2 CH.sub.3 phenyl t-butoxycarbonylamine                           353 NHSO.sub.2 CH.sub.3 phenyl (N-pyrrolidino)formylimino                      354 NHSO.sub.2 CH.sub.3 phenyl (N-pyrrolidino)formyl-N-                           (methanesulfamoyl)imino                                                     355 NHSO.sub.2 CH.sub.3 2-F-phenyl guanidino                                   356 NHSO.sub.2 CH.sub.3 2-F-phenyl 2-thiazolin-2-ylamine                       357 NHSO.sub.2 CH.sub.3 2-F-phenyl N-methyl-2-imidazolin-2-yl                  358 NHSO.sub.2 CH.sub.3 2-F-phenyl N-methyl-1,4,5,6-                              tetrahydropyrimid-2-yl                                                      359 NHSO.sub.2 CH.sub.3 2-F-phenyl N-methylimidazol-2-ylthio                   360 NHSO.sub.2 CH.sub.3 2-F-phenyl t-butoxycarbonylamine                       361 NHSO.sub.2 CH.sub.3 2-F-phenyl (N-pyrrolidino)formylimino                  362 NHSO.sub.2 CH.sub.3 2-F-phenyl (N-pyrrolidino)formyl-N-                       (methanesulfamoyl)imino                                                     363 NHSO.sub.2 CH.sub.3 2-CH.sub.3 O-phenyl (N-pyrrolidino)formylimino                                   364 NHSO.sub.2 CH.sub.3 2-CH.sub.3 O-phenyl                                   (N-pyrrolidino)formyl-N-                                 (methanesulfamoyl)imino                                                   ______________________________________                                    

Utility

The compounds of this invention are useful as anticoagulants for the treatment or prevention of thromboembolic disorders in mammals. The term "thromboembolic disorders" as used herein includes arterial or venous cardiovascular or cerebrovascular thromboembolic disorders, including, for example, unstable angina, first or recurrent myocardial infarction, ischemic sudden death, transient ischemic attack, stroke, atherosclerosis, venous thrombosis, deep vein thrombosis, thrombophlebitis, arterial embolism, coronary and cerebral arterial thrombosis, cerebral embolism, kidney embolisms, and pulmonary embolisms. The anticoagulant effect of compounds of the present invention is believed to be due to inhibition of factor Xa or thrombin.

The effectiveness of compounds of the present invention as inhibitors of factor Xa was determined using purified human factor Xa and synthetic substrate. The rate of factor Xa hydrolysis of chromogenic substrate S2222 (Kabi Pharmacia, Franklin, Ohio) was measured both in the absence and presence of compounds of the present invention. Hydrolysis of the substrate resulted in the release of pNA, which was monitored spectrophotometrically by measuring the increase in absorbance at 405 nM. A decrease in the rate of absorbance change at 405 nm in the presence of inhibitor is indicative of enzyme inhibition. The results of this assay are expressed as inhibitory constant, K_(i).

Factor Xa determinations were made in 0.10 M sodium phosphate buffer, pH 7.5, containing 0.20 M NaCl, and 0.5% PEG 8000. The Michaelis constant, K_(m), for substrate hydrolysis was determined at 25° C. using the method of Lineweaver and Burk. Values of K_(i) were determined by allowing 0.2-0.5 nM human factor Xa (Enzyme Research Laboratories, South Bend, IN) to react with the substrate (0.20 mM-1 mM) in the presence of inhibitor. Reactions were allowed to go for 30 minutes and the velocities (rate of absorbance change vs time) were measured in the time frame of 25-30 minutes. The following relationship was used to calculate K_(i) values:

    (v.sub.o -v.sub.s)/v.sub.s =I/(K.sub.i (1+S/K.sub.m))

where:

v_(o) is the velocity of the control in the absence of inhibitor;

v_(s) is the velocity in the presence of inhibitor;

I is the concentration of inhibitor;

K_(i) is the dissociation constant of the enzyme:inhibitor complex;

S is the concentration of substrate;

K_(m) is the Michaelis constant.

Using the methodology described above, a number of compounds of the present invention were found to exhibit a K_(i) of ≦15 μM, thereby confirming the utility of the compounds of the present invention as effective Xa inhibitors.

The antithrombotic effect of compounds of the present invention can be demonstrated in a rabbit arterio-venous (AV) shunt thrombosis model. In this model, rabbits weighing 2-3 kg anesthetized with a mixture of xylazine (10 mg/kg i.m.) and ketamine (50 mg/kg i.m.) are used. A saline-filled AV shunt device is connected between the femoral arterial and the femoral venous cannulae. The AV shunt device consists of a piece of 6-cm tygon tubing which contains a piece of silk thread. Blood will flow from the femoral artery via the AV-shunt into the femoral vein. The exposure of flowing blood to a silk thread will induce the formation of a significant thrombus. After forty minutes, the shunt is disconnected and the silk thread covered with thrombus is weighed. Test agents or vehicle will be given (i.v., i.p., s.c., or orally) prior to the opening of the AV shunt. The percentage inhibition of thrombus formation is determined for each treatment group. The ID50 values (dose which produces 50% inhibition of thrombus formation) are estimated by linear regression.

The compounds of formula (I) may also be useful as inhibitors of serine proteases, notably human thrombin, plasma kallikrein and plasmin. Because of their inhibitory action, these compounds are indicated for use in the prevention or treatment of physiological reactions, blood coagulation and inflammation, catalyzed by the aforesaid class of enzymes. Specifically, the compounds have utility as drugs for the treatment of diseases arising from elevated thrombin activity such as myocardial infarction, and as reagents used as anticoagulants in the processing of blood to plasma for diagnostic and other commercial purposes.

Some compounds of the present invention were shown to be direct acting inhibitors of the serine protease thrombin by their ability to inhibit the cleavage of small molecule substrates by thrombin in a purified system. In vitro inhibition constants were determined by the method described by Kettner et al. in J. Biol. Chem. 265, 18289-18297 (1990), herein incorporated by reference. In these assays, thrombin-mediated hydrolysis of the chromogenic substrate S2238 (Helena Laboratories, Beaumont, Tex.) was monitored spectrophotometrically. Addition of an inhibitor to the assay mixture results in decreased absorbance and is indicative of thrombin inhibition. Human thrombin (Enzyme Research Laboratories, Inc., South Bend, Ind.) at a concentration of 0.2 nM in 0.10 M sodium phosphate buffer, pH 7.5, 0.20 M NaCl, and 0.5% PEG 6000, was incubated with various substrate concentrations ranging from 0.20 to 0.02 mM. After 25 to 30 minutes of incubation, thrombin activity was assayed by monitoring the rate of increase in absorbance at 405 nm which arises owing to substrate hydrolysis. Inhibition constants were derived from reciprocal plots of the reaction velocity as a function of substrate concentration using the standard method of Lineweaver and Burk. Using the methodology described above, some compounds of this invention were evaluated and found to exhibit a K_(i) of less than 15 μm, thereby confirming the utility of the compounds of the present invention as effective Xa inhibitors.

The compounds of the present invention can be administered alone or in combination with one or more additional therapeutic agents. These include other anti-coagulant or coagulation inhibitory agents, anti-platelet or platelet inhibitory agents, thrombin inhibitors, or thrombolytic or fibrinolytic agents.

The compounds are administered to a mammal in a therapeutically effective amount. By "therapeutically effective amount" it is meant an amount of a compound of Formula I that, when administered alone or in combination with an additional therapeutic agent to a mammal, is effective to prevent or ameliorate the thromboembolic disease condition or the progression of the,disease.

By "administered in combination" or "combination therapy" it is meant that the compound of Formula I and one or more additional therapeutic agents are administered concurrently to the mammal being treated. When administered in combination each component may be administered at the same time or sequentially in any order at different points in time. Thus, each component may be administered separately but sufficiently closely in time so as to provide the desired therapeutic effect. Other anticoagulant agents (or coagulation inhibitory agents) that may be used in combination with the compounds of this invention include warfarin and heparin, as well as other factor Xa inhibitors such as those described in the publications identified above under Background of the Invention.

The term anti-platelet agents (or platelet inhibitory agents), as used herein, denotes agents that inhibit platelet function such as by inhibiting the aggregation, adhesion or granular secretion of platelets. Such agents include, but are not limited to, the various known non-steroidal anti-inflammatory drugs (NSAIDS) such as aspirin, ibuprofen, naproxen, sulindac, indomethacin, mefenamate, droxicam, diclofenac, sulfinpyrazone, and piroxicam, including pharmaceutically acceptable salts or prodrugs thereof. Of the NSAIDS, aspirin (acetylsalicyclic acid or ASA), and piroxicam are preferred. Other suitable anti-platelet agents include ticlopidine, including pharmaceutically acceptable salts or prodrugs thereof. Ticlopidine is also a preferred compound since it is known to be gentle on the gastro-intestinal tract in use. Still other suitable platelet inhibitory agents include IIb/IIIa antagonists, thromboxane-A2-receptor antagonists and thromboxane-A2-synthetase inhibitors, as well as pharmaceutically acceptable salts or prodrugs thereof.

The term thrombin inhibitors (or anti-thrombin agents), as used herein, denotes inhibitors of the serine protease thrombin. By inhibiting thrombin, various thrombin-mediated processes, such as thrombin-mediated platelet activation (that is, for example, the aggregation of platelets, and/or the granular secretion of plasminogen activator inhibitor-1 and/or serotonin) and/or fibrin formation are disrupted. A number of thrombin inhibitors are known to one of skill in the art and these inhibitors are contemplated to be used in combination with the present compounds. Such inhibitors include, but are not limited to, boroarginine derivatives, boropeptides, heparins, hirudin and argatroban, including pharmaceutically acceptable salts and prodrugs thereof. Boroarginine derivatives and boropeptides include N-acetyl and peptide derivatives of boronic acid, such as C-terminal a-aminoboronic acid derivatives of lysine, ornithine, arginine, homoarginine and corresponding isothiouronium analogs thereof. The term hirudin, as used herein, includes suitable derivatives or analogs of hirudin, referred to herein as hirulogs, such as disulfatohirudin. Boropeptide thrombin inhibitors include compounds described in Kettner et al., U.S. Pat. No. 5,187,157 and European Patent Application Publication Number 293 881 A2, the disclosures of which are hereby incorporated herein by reference. Other suitable boroarginine derivatives and boropeptide thrombin inhibitors include those disclosed in PCT Application Publication Number 92/07869 and European Patent Application Publication Number 471,651 A2, the disclosures of which are hereby incorporated herein by reference.

The term thrombolytics (or fibrinolytic) agents (or thrombolytics or fibrinolytics), as used herein, denotes agents that lyse blood clots (thrombi). Such agents include tissue plasminogen activator, anistreplase, urokinase or streptokinase, including pharmaceutically acceptable salts or prodrugs thereof. The term anistreplase, as used herein, refers to anisoylated plasminogen streptokinase activator complex, as described, for example, in European Patent Application No. 028,489, the disclosure of which is hereby incorporated herein by reference herein. The term urokinase, as used herein, is intended to denote both dual and single chain urokinase, the latter also being referred to herein as prourokinase.

Administration of the compounds of Formula I of the invention in combination with such additional therapeutic agent, may afford an efficacy advantage over the compounds and agents alone, and may do so while permitting the use of lower doses of each. A lower dosage minimizes the potential of side effects, thereby providing an increased margin of safety.

The compounds of the present invention are also useful as standard or reference compounds, for example as a quality standard or control, in tests or assays involving the inhibition of factor Xa. Such compounds may be provided in a commercial kit, for example, for use in pharmaceutical research involving factor Xa. For example, a compound of the present invention could be used as a reference in an assay to compare its known activity to a compound with an unknown activity. This would ensure the experimenter that the assay was being performed properly and provide a basis for comparison, especially if the test compound was a derivative of the reference compound. When developing new assays or protocols, compounds according to the present invention could be used to test their effectiveness.

The compounds of the present invention may also be used in diagnostic assays involving factor Xa. For example, the presence of factor Xa in an unknown sample could be determined by addition of chromogenic substrate S2222 to a series of solutions containing test sample and optionally one of the compounds of the present invention. If production of pNA is observed in the solutions containing test sample, but no compound of the present invention, then one would conclude factor Xa was present.

Dosage and Formulation

The compounds of this invention can be administered in such oral dosage forms as tablets, capsules (each of which includes sustained release or timed release formulations), pills, powders, granules, elixirs, tinctures, suspensions, syrups, and emulsions. They may also be administered in intravenous (bolus or infusion), intraperitoneal, subcutaneous, or intramuscular form, all using dosage forms well known to those of ordinary skill in the pharmaceutical arts. They can be administered alone, but generally will be administered with a pharmaceutical carrier selected on the basis of the chosen route of administration and standard pharmaceutical practice.

The dosage regimen for the compounds of the present invention will, of course, vary depending upon known factors, such as the pharmacodynamic characteristics of the particular agent and its mode and route of administration; the species, age, sex, health, medical condition, and weight of the recipient; the nature and extent of the symptoms; the kind of concurrent treatment; the frequency of treatment; the route of administration, the renal and hepatic function of the patient,and the effect desired. A physician or veterinarian can determine and prescribe the effective amount of the drug required to prevent, counter, or arrest the progress of the thromboembolic disorder.

By way of general guidance, the daily oral dosage of each active ingredient, when used for the indicated effects, will range between about 0.001 to 1000 mg/kg of body weight, preferably between about 0.01 to 100 mg/kg of body weight per day, and most preferably between about 1.0 to 20 mg/kg/day. Intravenously, the most preferred doses will range from about 1 to about 10 mg/kg/minute during a constant rate infusion. Compounds of this invention may be administered in a single daily dose, or the total daily dosage may be administered in divided doses of two, three, or four times daily.

Compounds of this invention can be administered in intranasal form via topical use of suitable intranasal vehicles, or via transdermal routes, using transdermal skin patches. When administered in the form of a transdermal delivery system, the dosage administration will, of course, be continuous rather than intermittent throughout the dosage regimen.

The compounds are typically administered in admixture with suitable pharmaceutical diluents, excipients, or carriers (collectively referred to herein as pharmaceutical carriers) suitably selected with respect to the intended form of administration, that is, oral tablets, capsules, elixirs, syrups and the like, and consistent with conventional pharmaceutical practices.

For instance, for oral administration in the form of a tablet or capsule, the active drug component can be combined with an oral, non-toxic, pharmaceutically acceptable, inert carrier such as lactose, starch, sucrose, glucose, methyl callulose, magnesium stearate, dicalcium phosphate, calcium sulfate, mannitol, sorbitol and the like; for oral administration in liquid form, the oral drug components can be combined with any oral, non-toxic, pharmaceutically acceptable inert carrier such as ethanol, glycerol, water, and the like. Moreover, when desired or necessary, suitable binders, lubricants, disintegrating agents, and coloring agents can also be incorporated into the mixture. Suitable binders include starch, gelatin, natural sugars such as glucose or beta-lactose, corn sweeteners, natural and synthetic gums such as acacia, tragacanth, or sodium alginate, carboxymethylcellulose, polyethylene glycol, waxes, and the like. Lubricants used in these dosage forms include sodium oleate, sodium stearate, magnesium stearate, sodium benzoate, sodium acetate, sodium chloride, and the like. Disintegrators include, without limitation, starch, methyl cellulose, agar, bentonite, xanthan gum, and the like.

The compounds of the present invention can also be administered in the form of liposome delivery systems, such as small unilamellar vesicles, large unilamellar vesicles, and multilamellar vesicles. Liposomes can be formed from a variety of phospholipids, such as cholesterol, stearylamine, or phosphatidylcholines.

Compounds of the present invention may also be coupled with soluble polymers as targetable drug carriers. Such polymers can include polyvinylpyrrolidone, pyran copolymer, polyhydroxypropylmethacrylamide-phenol, polyhydroxyethylaspartamidephenol, or polyethyleneoxidepolylysine substituted with palmitoyl residues. Furthermore, the compounds of the present invention may be coupled to a class of biodegradable polymers useful in achieving controlled release of a drug, for example, polylactic acid, polyglycolic acid, copolymers of polylactic and polyglycolic acid, polyepsilon caprolactone, polyhydroxy butyric acid, polyorthoesters, polyacetals, polydihydropyrans, polycyanoacylates, and crosslinked or amphipathic block copolymers of hydrogels.

Dosage forms (pharmaceutical compositions) suitable for administration may contain from about 1 milligram to about 100 milligrams of active ingredient per dosage unit. In these pharmaceutical compositions the active ingredient will ordinarily be present in an amount of about 0.5-95% by weight based on the total weight of the composition.

Gelatin capsules may contain the active ingredient and powdered carriers, such as lactose, starch, cellulose derivatives, magnesium stearate, stearic acid, and the like. Similar diluents can be used to make compressed tablets. Both tablets and capsules can be manufactured as sustained release products to provide for continuous release of medication over a period of hours. Compressed tablets can be sugar coated or film coated to mask any unpleasant taste and protect the tablet from the atmosphere, or enteric coated for selective disintegration in the gastrointestinal tract.

Liquid dosage forms for oral administration can contain coloring and flavoring to increase patient acceptance.

In general, water, a suitable oil, saline, aqueous dextrose (glucose), and related sugar solutions and glycols such as propylene glycol or polyethylene glycols are suitable carriers for parenteral solutions. Solutions for parenteral administration preferably contain a water soluble salt of the active ingredient, suitable stabilizing agents, and if necessary, buffer substances. Antioxidizing agents such as sodium bisulfite, sodium sulfite, or ascorbic acid, either alone or combined, are suitable stabilizing agents. Also used are citric acid and its salts and sodium EDTA. In addition, parenteral solutions can contain preservatives, such as benzalkonium chloride, methyl- or propyl-paraben, and chlorobutanol.

Suitable pharmaceutical carriers are described in Remington's Pharmaceutical Sciences, Mack Publishing Company, a standard reference text in this field.

Representative useful pharmaceutical dosage-forms for administration of the compounds of this invention can be illustrated as follows:

Capsules

A large number of unit capsules can be prepared by filling standard two-piece hard gelatin capsules each with 100 milligrams of powdered active ingredient, 150 milligrams of lactose, 50 milligrams of cellulose, and 6 milligrams magnesium stearate.

Soft Gelatin Capsules

A mixture of active ingredient in a digestable oil such as soybean oil, cottonseed oil or olive oil may be prepared and injected by means of a positive displacement pump into gelatin to form soft gelatin capsules containing 100 milligrams of the active ingredient. The capsules should be washed and dried.

Tablets

Tablets may be prepared by conventional procedures so that the dosage unit is 100 milligrams of active ingredient, 0.2 milligrams of colloidal silicon dioxide, 5 milligrams of magnesium stearate, 275 milligrams of microcrystalline cellulose, 11 milligrams of starch and 98.8 milligrams of lactose. Appropriate coatings may be applied to increase palatability or delay absorption.

Injectable

A parenteral composition suitable for administration by injection may be prepared by stirring 1.5% by weight of active ingredient in 10% by volume propylene glycol and water. The solution should be made isotonic with sodium chloride and sterilized.

Suspension

An aqueous suspension can be prepared for oral administration so that each 5 mL contain 100 mg of finely divided active ingredient, 200 mg of sodium carboxymethyl cellulose, 5 mg of sodium benzoate, 1.0 g of sorbitol solution, U.S.P., and 0.025 mL of vanillin.

Where the compounds of this invention are combined with other anticoagulant agents, for example, a daily dosage may be about 0.1 to 100 milligrams of the compound of Formula I and about 1 to 7.5 milligrams of the second anticoagulant, per kilogram of patient body weight. For a tablet dosage form, the compounds of this invention generally may be present in an amount of about 5 to 10 milligrams per dosage unit, and the second anti-coagulant in an amount of about 1 to 5 milligrams per dosage unit.

Where the compounds of Formula I are administered in combination with an anti-platelet agent, by way of general guidance, typically a daily dosage may be about 0.01 to 25 milligrams of the compound of Formula I and about 50 to 150 milligrams of the anti-platelet agent, preferably about 0.1 to 1 milligrams of the compound of Formula I and about 1 to 3 milligrams of antiplatelet agents, per kilogram of patient body weight.

Where the compounds of Formula I are adminstered in combination with thrombolytic agent, typically a daily dosage may be about 0.1 to 1 milligrams of the compound of Formula I, per kilogram of patient body weight and, in the case of the thrombolytic agents, the usual dosage of the thrombolyic agent when administered alone may be reduced by about 70-80% when administered with a compound of Formula I.

Where two or more of the foregoing second therapeutic agents are administered with the compound of Formula I, generally the amount of each component in a typical daily dosage and typical dosage form may be reduced relative to the usual dosage of the agent when administered alone, in view of the additive or synergistic effect of the therapeutic agents when administered in combination.

Particularly when provided as a single dosage unit, the potential exists for a chemical interaction between the combined active ingredients. For this reason, when the compound of Formula I and a second therapeutic agent are combined in a single dosage unit they are formulated such that although the active ingredients are combined in a single dosage unit, the physical contact between the active ingredients is minimized (that is, reduced). For example, one active ingredient may be enteric coated. By enteric coating one of the active ingredients, it is possible not only to minimize the contact between the combined active ingredients, but also, it is possible to control the release of one of these components in the gastrointestinal tract such that one of these components is not released in the stomach but rather is released in the intestines. One of the active ingredients may also be coated with a material which effects a sustained-release throughout the gastrointestinal tract and also serves to minimize physical contact between the combined active ingredients. Furthermore, the sustained-released component can be additionally enteric coated such that the release of this component occurs only in the intestine. Still another approach would involve the formulation of a combination product in which the one component is coated with a sustained and/or enteric release polymer, and the other component is also coated with a polymer such as a lowviscosity grade of hydroxypropyl methylcellulose (HPMC) or other appropriate materials as known in the art, in order to further separate the active components. The polymer coating serves to form an additional barrier to interaction with the other component.

These as well as other ways of minimizing contact between the components of combination products of the present invention, whether administered in a single dosage form or administered in separate forms but at the same time by the same manner, will be readily apparent to those skilled in the art, once armed with the present disclosure.

Obviously, numerous modifications and variations of the present invention are possible in light of the above teachings. It is therefore to be understood that within the scope of the appended claims, the invention may be practiced otherwise that as specifically described herein. 

What is claimed is:
 1. A compound of formula I: ##STR212## or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein;ring M contains from 0-1 N atoms; D is selected from CN, C(═NR⁷)NR⁸ R⁹, NHC(═NR⁷)NR⁸ R⁹, NR⁸ CH(═NR⁷), C(O)NR⁸ R⁹, and (CR⁸ R⁹)_(t) NR⁸ R⁹ ; E is selected from phenyl, 2-pyridyl, 4-pyridyl, pyrimidyl, and piperidinyl substituted with 1 R; R is selected from H, F, Cl, Br, I, OR³, SR³, CO₂ R³, NO₂, and CH₂ OR³, and (CR⁸ R⁹)_(t) NR⁸ R⁹ ; with the proviso that if t is equal to 0 and E is selected from phenyl, then R is selected from F, Cl, Br, and I; alternatively, E and R combine to form methylenedioxy or ethylenedioxy; Z is selected from a bond, C₁₋₄ alkylene, (CH₂)_(r) O(CH₂)_(r), (CH₂)_(r) NR³ (CH₂)_(r), (CH₂)_(r) C(O) (CH₂)_(r), (CH₂)_(r) C(O)O(CH₂)_(r), (CH₂)_(r) OC(O)(CH₂)_(r), (CH₂)_(r) C(O)NR³ (CH₂)_(r), (CH₂)_(r) NR³ C(O)(CH₂)_(r), (CH₂)_(r) OC(O)O(CH₂)_(r), (CH₂)_(r) OC(O)NR³ (CH₂)_(r), (CH₂)_(r) NR³ C(O)O(CH₂)_(r), (CH₂)_(r) NR³ C(O)NR³ (CH₂)_(r), (CH₂)_(r) S(O)_(p) (CH₂)_(r), (CH₂)_(r) SO₂ NR³ (CH₂)_(r), (CH₂)_(r) NR³ S02(CH₂)_(r), and (CH₂)_(r) NR³ SO₂ NR³ (CH₂)_(r), provided that Z does not form a N--N, N--O, N--S, NCH₂ N, NCH₂ O, or NCH₂ S bond with ring M or group A; R^(1a) and R^(1b) are independently absent or selected from --(CH₂)_(r) --R^(1'), --CH═CH--R^(1'), NCH₂ R^(1"), OCH₂ R^(1"), SCH₂ R^(1"), NH(CH₂)₂ (CH₂)_(t) R^(1'), O(CH₂)₂ (CH₂)_(t) R^(1'), and S(CH₂)₂ (CH₂)_(t) R^(1') ; alternatively, R^(1a) and R^(1b), when attached to adjacent carbon atoms, together with the atoms to which they are attached form a 5-8 membered saturated, partially saturated or unsaturated ring substituted with 0-2 R⁴ and which contains from 0-2 heteroatoms selected from the group consisting of N, O, and S; alternatively, when Z is C(O)NH and R^(1a) is attached to a ring carbon adjacent to Z, then R^(1a) is a C(O) which replaces the amide hydrogen of Z to form a cyclic imide; R^(1') is selected from H, C₁₋₃ alkyl, F, Cl, Br, I, --CN, --CHO, (CF₂)_(r) CF₃, (CH₂)_(r) OR², NR² R^(2a), C(O) R^(2c), OC(O)R², (CF₂)_(r) CO₂ R^(2c), S(O)_(p) R^(2b), NR² (CH₂)_(r) OR², CH(═NR^(2c))NR² R^(2a), NR² C(O)R^(2b), NR² C(O)NHR^(2b), NR² C(O)₂ R^(2a), OC(O)NR^(2a) R^(2b), C(O)NR² R^(2a), C(O)NR² (CH₂)_(r) OR², SO₂ NR² R^(2a), NR² SO₂ R^(2b), C₃₋₆ carbocyclic residue substituted with 0-2 R⁴, and 5-10 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R⁴ ; R^(1") is selected from H, CH(CH₂ OR²)₂, C(O)R^(2c), C(O)NR² R^(2a), S(O)R^(2b), S(O)₂ R^(2b), and SO₂ NR² R^(2a) ; R², at each occurrence, is selected from H, CF₃, C₁₋₆ alkyl, benzyl, C₃₋₆ carbocyclic residue substituted with 0-2 R^(4b), and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R^(4b) ; R^(2a), at each occurrence, is selected from H, CF₃, C₁₋₆ alkyl, benzyl, phenethyl, C₃₋₆ carbocyclic residue substituted with 0-2 R^(4b), and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R^(4b) ; R^(2b), at each occurrence, is selected from CF₃, C₁₋₄ alkoxy, C₁₋₆ alkyl, benzyl, C₃₋₆ carbocyclic residue substituted with 0-2 R^(4b), and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R^(4b) ; R^(2c), at each occurrence, is selected from CF₃, OH, C₁₋₄ alkoxy, C₁₋₆ alkyl, benzyl, C₃₋₆ carbocyclic residue substituted with 0-2 R^(4b), and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R^(4b) ; alternatively, R² and R^(2a), together with the atom to which they are attached, combine to form a 5 or 6 membered saturated, partially saturated or unsaturated ring substituted with 0-2 R^(4b) and containing from 0-1 additional heteroatoms selected from the group consisting of N, O, and S; R³, at each occurrence, is selected from H, C₁₋₄ alkyl, and phenyl; R^(3a), at each occurrence, is selected from H, C₁₋₄ alkyl, and phenyl; R^(3b), at each occurrence, is selected from H, C₁₋₄ alkyl, and phenyl; R^(3c), at each occurrence, is selected from C₁₋₄ alkyl, and phenyl; A is selected from:C₃₋₁₀ carbocyclic residue substituted with 0-2 R⁴[, and - 10membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R⁴ ]; B is selected from: H, Y, and X--Y; X is selected from C₁₋₄ alkylene, --CR² (CR² R^(2b))(CH₂)_(t) --, --C(O)--, --C(═NR^(1"))--, --CR² (NR^(1") R²)--, --CR² (OR²)--, --CR² (SR²)--, --C(O)CR² R^(2a) --, --CR² R^(2a) C(O), --S(O)_(p) --, --S(O)_(p) CR² R^(2a) --, --CR² R^(2a) S(O)_(p) --, --S(O)₂ NR² --, --NR² S(O)₂ --, --NR² S(O)₂ CR² R^(2a) --, --CR² R^(2a) S(O)₂ NR² --, --NR² S(O)₂ NR² --, --C(O)NR² --, --NR² C(O)--, --C(O)NR^(2c) R² R^(2a) --, --NR² C(O)CR² R^(2a) --, --CR² R^(2a) C(O)NR² --, --CR² R^(2a) NR² C(O)--, --NR² C(O)O--, --OC(O)NR² --, --NR² C(O)NR² --, --NR² --, --NR^(2c) R² R^(2a) --, --CR² R^(2a) NR² --, O, --CR² R^(2a) O--, and --OCR² R^(2a) --; Y is selected from:(CH₂)_(r) NR² R^(2a), provided that X--Y do not form a N--N, O--N, or S--N bond, C₃₋₁₀ carbocyclic residue substituted with 0-2 R^(4a), and 5-10 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R^(4a) ; R⁴, at each occurrence, is selected from H, ═O, (CH₂)_(r) OR², F, Cl, Br, I, C₁₋₄ alkyl, --CN, NO₂, (CH₂)_(r) NR² R^(2a), (CH₂)_(r) C(O)R^(2c), NR² C(O)R^(2b), C(O)NR² R^(2a), NR² C(O)NR² R^(2a), CH(═NR²)NR² R^(2a), CH(═NS(O)₂ R⁵)NR² R^(2a), NHC(═NR²)NR² R^(2a), C(O)NHC(═NR²)NR² R^(2a), SO₂ NR² R^(2a), NR² SO₂ NR² R^(2a), NR² SO₂ -C₁₋₄ alkyl, NR² SO₂ R⁵, S(O)_(p) R⁵, (CF₂)_(r) CF₃, NCH₂ R^(1"), OCH₂ R^(1"), SCH₂ R^(1"), N(CH₂)₂ (CH₂)_(t) R^(1'), O(CH₂)₂ (CH₂)_(t) R^(1'), and S(CH₂)₂ (CH₂)_(t) R^(1') ; alternatively, one R⁴ is a 5-6 membered aromatic heterocycle containing from 1-4 heteroatoms selected from the group consisting of N, O, and S; R^(4a), at each occurrence, is selected from H, ═O, (CH₂)_(r) OR², (CH₂)_(r) --F, (CH₂)_(r) --Br, (CH₂)_(r) --Cl, I, C₁₋₄ alkyl, --CN, NO₂, (CH₂) rNR² R^(2a), (CH₂)_(r) NR² R^(2b), (CH₂)_(r) C(O)R^(2c), NR² C(O)R^(2b), C(O)NR² R^(2a), C(O)NH(CH₂)₂ NR² R^(2a), NR² C(O)NR² R^(2a), CH(═NR²)NR² R^(2a), NHC(═NR²)NR² R^(2a), SO₂ NR² R^(2a), NR² SO₂ NR² SO₂ R⁵, NR² SO₂ --C₁₋₄ alkyl, C(O)NHSO₂ --C₁₋₄ alkyl, NR² SO₂ R⁵, S(O)_(p) R⁵, and (CF₂)_(r) CF₃ ; alternatively, one R^(4a) is a 5-6 membered aromatic heterocycle containing from 1-4 heteroatoms selected from the group consisting of N, O, and S and substituted with 0-1 R⁵ ; R^(4b), at each occurrence, is selected from H, ═O, (CH₂)_(r) OR³, F, Cl, Br, I, C₁₋₄ alkyl, --CN, NO₂, (CH₂)_(r) NR³ R^(3a), (CH₂)_(r) C(O)R³, (CH₂)_(r) C(O)OR^(3c), NR³ C(O)R^(3a), C(O)NR³ R^(3a), NR³ C(O)NR³ R^(3a), CH(═NR³)NR³ R^(3a), NH³ C(═NR³)NR³ R^(3a), SO₂ NR³ R^(3a), NR³ SO₂ NR³ R^(3a), NR³ SO₂ -C₁₋₄ alkyl, NR³ SO₂ CF₃, NR³ SO₂ -phenyl, S(O)_(p) CF₃, S(O)_(p) -C₁₋₄ alkyl, S(O)_(p) -phenyl, and (CF₂)_(r) CF₃ ; R⁵, at each occurrence, is selected from CF₃, C₁₋₆ alkyl, phenyl substituted with 0-2 R⁶, and benzyl substituted with 0-2 R⁶ ; R⁶, at each occurrence, is selected from H, OH, (CH₂)_(r) OR², F, Cl, Br, I, C₁₋₄ alkyl, CN, NO₂, (CH₂)_(r) NR² R^(2a), (CH₂)_(r) C(O)R^(2b), NR² C(O)R^(2b), NR² C(O)NR² R^(2a), CH(═NH)NH₂, NHC(═NH)NH₂, SO₂ NR² R^(2a), NR² SO₂ NR² R^(2a), and NR² SO₂ C₁₋₄ alkyl; R⁷, at each occurrence, is selected from H, OH, C₁₋₆ alkyl, C₁₋₆ alkylcarbonyl, C₁₋₆ alkoxy, C₁₋₄ alkoxycarbonyl, (CH₂)_(n) -phenyl, C₆₋₁₀ aryloxy, C₆₋₁₀ aryloxycarbonyl, C₆₋₁₀ arylmethylcarbonyl, C₁₋₄ alkylcarbonyloxy C₁₋₄ alkoxycarbonyl, C₆₋₁₀ arylcarbonyloxy C₁₋₄ alkoxycarbonyl, C₁₋₆ alkylaminocarbonyl, phenylaminocarbonyl, and phenyl-C₁₋₄ alkoxycarbonyl; R⁸, at each occurrence, is selected from H, C₁₋₆ alkyl and (CH₂)_(n) -phenyl; alternatively, R⁷ and R⁸ combine to form a 5 or 6 membered saturated, ring which contains from 0-1 additional heteroatoms selected from the group consisting of N, O, and S; R⁹, at each occurrence, is selected from H, C₁₋₆ alkyl and (CH₂)_(n) -phenyl; n is selected from 0, 1, 2, and 3; m is selected from 0, 1, and 2; p is selected from 0, 1, and 2; r is selected from 0, 1, 2, and 3; s is selected from 0, 1, and 2; and, t is selected from 0 and
 1. 2. A compound according to claim 1, wherein is of formulae Ia-Ie: ##STR213## wherein: Z is selected from a bond, CH₂ O, OCH₂, CH₂ NH, NHCH₂, CH₂ C(O), C(O)CH₂, C(O)NH, C(O)NH, CH₂ S(O)₂, S(O)₂ (CH₂), SO₂ NH, and SO₂ NH;B is selected from: Y, X--Y, and NR² R^(2a) ; Y is selected from one of the following carbocyclic and heterocyclic systems which are substituted with 0-2 R^(4a) ;phenyl, piperidinyl, piperazinyl, pyridyl, pyrimidyl, furanyl, morpholinyl, thiophenyl, pyrrolyl, pyrrolidinyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, oxadiazole, thiadiazole, triazole, 1,2,3-oxadiazole, 1,2,4-oxadiazole, 1,2,5-oxadiazole, 1,3,4-oxadiazole, 1,2,3-thiadiazole, 1,2,4-thiadiazole, 1,2,5-thiadiazole, 1,3,4-thiadiazole, 1,2,3-triazole, 1,2,4-triazole, 1,2,5-triazole, 1,3,4-triazole, benzofuran, benzothiofuran, indole, benzimidazole, benzoxazole, benzthiazole, indazole, benzisoxazole, benzisothiazole, and isoindazole; Y may also be selected from the following bicyclic heteroaryl ring systems: ##STR214## K is selected from O, S, NH, and N.
 3. A compound according to claim 2, wherein is of formulae: ##STR215## wherein: D is selected from C(═NR⁷)NR⁸ R⁹ and (CR⁸ R⁹)_(t) NR⁸ R⁹ ;R is selected from H, F, Cl, OR³, CH₂ OR³, CH₂ NH₂ ; A is selected from:C₅₋₆ carbocyclic residue substituted with 0-2 R⁴ ; Y is selected from one of the following carbocyclic and heterocyclic systems which are substituted with 0-2 R^(4a) ;phenyl, piperidinyl, piperazinyl, pyridyl, pyrimidyl, furanyl, morpholinyl, thiophenyl, pyrrolyl, pyrrolidinyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, benzimidazolyl, oxadiazole, thiadiazole, triazole, 1,2,3-oxadiazole, 1,2,4-oxadiazole, 1,2,5-oxadiazole, 1,3,4-oxadiazole, 1,2,3-thiadiazole, 1,2,4-thiadiazole, 1,2,5-thiadiazole, 1,3,4-thiadiazole, 1,2,3-triazole, 1,2,4-triazole, 1,2,5-triazole, and 1,3,4-triazole.
 4. A compound according to claim 3, wherein:E is phenyl; D is selected from C(═NH)NH₂ and CH₂ NH₂ ; R is selected from H, F, Cl, and Br; A is selected from:C₅₋₆ carbocyclic residue substituted with 0-2 R⁴ ; Y is selected from one of the following carbocyclic and heterocyclic systems which are substituted with 0-2 R^(4a) ;phenyl, piperidinyl, piperazinyl, pyridyl, pyrimidyl, furanyl, morpholinyl, thiophenyl, pyrrolyl, pyrrolidinyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, benzimidazolyl, oxadiazole, thiadiazole, triazole, 1,2,3-oxadiazole, 1,2,4-oxadiazole, 1,2,5-oxadiazole, 1,3,4-oxadiazole, 1,2,3-thiadiazole, 1,2,4-thiadiazole, 1,2,5-thiadiazole, 1,3,4-thiadiazole, 1,2,3-triazole, 1,2,4-triazole, 1,2,5-triazole, and 1,3,4-triazole; R², at each occurrence, is selected from H, CF₃, C₁₋₆ alkyl, benzyl, C₅₋₆ carbocyclic residue substituted with 0-2 R^(4b), and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R^(4b) ; R^(2a), at each occurrence, is selected from H, CF₃, C₁₋₆ alkyl, benzyl, phenethyl, C₅₋₆ carbocyclic residue substituted with 0-2 R^(4b), and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R^(4b) ; R^(2b), at each occurrence, is selected from CF₃, C₁₋₄ alkoxy, C₁₋₆ alkyl, benzyl, C₅₋₆ carbocyclic residue substituted with 0-2 R^(4b), and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R^(4b) ; R^(2c), at each occurrence, is selected from CF₃, OH, C₁₋₄ alkoxy, C₁₋₆ alkyl, benzyl, C₅₋₆ carbocyclic residue substituted with 0-2 R^(4b), and 5-6 membered heterocyclic system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S substituted with 0-2 R^(4b) ; alternatively, R² and R^(2a), together with the atom to which they are attached, combine to form a ring selected from imidazolyl, morpholino, piperazinyl, pyridyl, and pyrrolidinyl, substituted with 0-2 R^(4b) ; R⁴, at each occurrence, is selected from H, ═O, OR², CH₂ OR², F, Cl, C₁₋₄ alkyl, NR² R^(2a), CH₂ NR² R^(2a), C(O)R^(2c), CH₂ C(O)R^(2c), C(O)NR² R^(2a), CH(═NR²)NR² R^(2a), CH(═NS(O)₂ R⁵)NR² R^(2a), SO₂ NR² R^(2a), NR² SO₂ -C₁₋₄ alkyl, S(O)₂ R⁵, and CF₃ provided that if B is H, then R⁴ is other than tetrazole, C(O)-alkoxy, and C(O)NR² R^(2a) ; R^(4a), at each occurrence, is selected from H, ═O, (CH₂)_(r) OR², F, Cl, C₁₋₄ alkyl, NR² R^(2a), CH₂ NR² R^(2a), NR² R^(2b), CH₂ NR² R^(2b), (CH₂)_(r) C(O)R^(2c), NR² C(O) R^(2b), C(O) NR² R^(2a), C(O)NH(CH₂)₂ NR² R^(2a), NR² C(O)NR² R^(2a), SO₂ NR² R^(2a), S(O)₂ R⁵, and CF₃ ; and, R^(4b), at each occurrence, is selected from H, ═O, (CH₂)_(r) OR³, F, Cl, C₁₋₄ alkyl, NR³ R^(3a), CH₂ NR³ R^(3a), C(O)R³, CH₂ C(O)R³, C(O)OR^(3c), C(O)NR³ R^(3a), CH(═NR³)NR³ R^(3a), SO₂ NR³ R^(3a), NR³ SO₂ -C₁₋₄ alkyl, NR³ SO₂ CF₃, NR³ SO₂ -phenyl, S(O)₂ CF₃, S(O)₂ -C₁₋₄ alkyl, S(O)₂ -phenyl, and CF₃.
 5. A compound according to claim 1, wherein the compound is selected from:N-(2'-Aminosulfonyl-[1,1']biphen-4-yl)-2-(3'-amidinophenyl)nicotinamide; N-[5-(2-aminosulfonyl)phenylpyrid-2-yl]-2-(3'-amidinophenyl)nicotinamide; N-[5-(2-t-butylaminosulfonyl)phenylpyrid-2-yl]-2-(3'-amidinophenyl)nicotinamide; and, N-[5-(2-aminosulfonyl)phenylpyrid-2-yl]-2-(3'-carboxamidophenyl)nicotinamide;or a pharmaceutically acceptable salt thereof.
 6. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound according to claim 1 or a pharmaceutically acceptable salt thereof.
 7. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound according to claim 2 or a pharmaceutically acceptable salt thereof.
 8. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound according to claim 3 or a pharmaceutically acceptable salt thereof.
 9. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound according to claim 4 or a pharmaceutically acceptable salt thereof.
 10. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound according to claim 5 or a pharmaceutically acceptable salt thereof.
 11. A method for treating or preventing a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound according to claim 1 or a pharmaceutically acceptable salt thereof.
 12. A method for treating or preventing a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound according to claim 2 or a pharmaceutically acceptable salt thereof.
 13. A method for treating or preventing a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound according to claim 3 or a pharmaceutically acceptable salt thereof.
 14. A method for treating or preventing a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound according to claim 4 or a pharmaceutically acceptable salt thereof.
 15. A method for treating or preventing a thromboembolic disorder, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound according to claim 5 or a pharmaceutically acceptable salt thereof. 